Search Result
Results for "
Mice model
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
18
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101194
-
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Tin-protoporphyrin IX; Sn-Protoporphyrin; SnPPIX
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Reactive Oxygen Species (ROS)
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Cancer
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Tin protoporphyrin IX dichloride (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin protoporphyrin IX dichloride sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model .
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- HY-N0745
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Caspase
ERK
Keap1-Nrf2
Heme Oxygenase (HO)
Apoptosis
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Neurological Disease
Inflammation/Immunology
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Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A) . Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury .
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- HY-120692
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JAK
STAT
Apoptosis
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Cancer
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Cyclanoline chloride is an alkaloid. Cyclanoline chloride can be isolated from Fangji. Cyclanoline (chloride) inhibits the phosphorylation of JAK2 and STAT3, and induces Apoptosis. Cyclanoline chloride suppresses tumor growth in subcutaneous bladder cancer xenograft models of nude mice. Cyclanoline chloride reverses cisplatin resistance in bladder cancer cells and enhances the efficacy of Cisplatin (HY-17394). Cyclanoline chloride can be used for research related to bladder cancer .
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- HY-P11058
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OVAp
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MHC
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Cancer
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OVA(250-264) (OVAvac) (OVAp) is an antigen peptide that can be from ovalbumin (OVA) presented by the class I MHC molecule, H-2Kb. OVA(250-264) combined withαMSLN (anti-MSLN antibody) significantly induces antigen-specific CD8 + T cell generation and infiltration for enhancing antitumor efficacy in orthotopic pancreatic cancer mice model. OVA(250-264) can be used for neoantigen vaccine development in pancreatic cancer immunotherapy research .
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- HY-111792
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CRX-601
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Toll-like Receptor (TLR)
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Inflammation/Immunology
Cancer
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GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. Not only, GSK1795091 inhibits tumor growth and increases the survival in mice model, but results in long term survival in influenza challenge model in mice .
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- HY-P10086
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Human TREM-1(213-221)
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TREM receptor
TNF Receptor
Interleukin Related
c-Fms
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Neurological Disease
Inflammation/Immunology
Cancer
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TREM-1 inhibitory peptide GF9 (Human TREM-1 (213-221)) is a TREM-1 inhibitor. TREM-1 inhibitory peptide GF9 blocks the TREM-1 signaling pathway via a ligand-independent mechanism, spontaneously inserts into the cell membrane to dissociate TREM-1 from DAP-12, and functions through the Signaling Chain Homooligomerization (SCHOOL) model. TREM-1 inhibitory peptide GF9 reduces the levels of TNFα, IL-1β, IL-6, and M-CSF. TREM-1 inhibitory peptide GF9 inhibits tumor growth, prolongs the survival of mice with pancreatic cancer models, ameliorates collagen-induced arthritis, and exerts protective effects on bone and cartilage simultaneously. TREM-1 inhibitory peptide GF9 can be used in research related to arthritis, pancreatic cancer, retinopathy, alcoholic liver disease, and liver cancer .
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- HY-174346
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E1/E2/E3 Enzyme
Apoptosis
DNA/RNA Synthesis
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Cancer
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Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38 μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research .
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- HY-P6084
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NOD-like Receptor (NLR)
p38 MAPK
Apoptosis
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Inflammation/Immunology
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RP-220 is a renalase peptide targeting NLRP3. RP220 has anti-inflammatory and anti-apoptotic activities. RP220 inhibits renal tubular epithelial cells apoptosis with alkaline insult by activating MAPK signaling pathway. RP220 significantly inhibits NLRP3 expression and reduces macrophage infiltration and kidney tissue damage in acute kidney injury (AKI) mice model. RP-220 can be uses for systemic lupus erythematosus (SLE) and its complication lupus nephritis (LN) research .
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- HY-N0469R
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Reference Standards
Endogenous Metabolite
Virus Protease
HSV
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Infection
Metabolic Disease
Inflammation/Immunology
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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- HY-126426
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DNA Methyltransferase
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Cardiovascular Disease
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CBHcy is an inhibitor for betaine-homocysteine S-methyltransferase (BGMT), with an IC50 of 0.09 μM. CBHcy upregulates the plasma total homocysteine and causes transient hyperhomocysteinemia in mice model .
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- HY-15266
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PRI 2202; Impurity D of Calcipotriol
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Drug Derivative
VD/VDR
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Cancer
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24R-Calcipotriol (PRI 2202; Impurity D of Calcipotriol), an isomer of Calcipotriol (HY-10001), is a synthetic vitamin D analog. 24R-Calcipotriol exhibits synergistic antiproliferative effects with low-dose cytostatics in in vitro. 24R-Calcipotriol produces tumor growth inhibition when combined with Cyclophosphamide (HY-17420) and Cisplatin (HY-17394) in mice models. 24R-Calcipotriol can increase serum calcium levels and reduce blood leukocyte counts . 24R-Calcipotriol can be used for the research of mammary cancer and Lewis lung cancer .
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- HY-122604
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DNA/RNA Synthesis
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Neurological Disease
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PF-DcpSi is a mRNA decapping scavenger enzyme (DcpS) inhibitor (IC50: 0.11 nM). PF-DcpSi (30 mg/kg,i.p.) ameliorates the disease phenotype in a mice model of spinal muscular atrophy (SMA) .
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- HY-12095
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Cannabinoid Receptor
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Neurological Disease
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CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
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- HY-176264
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SARS-CoV
Virus Protease
Cytochrome P450
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Infection
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DNDI-6510 (Compound (S)-x38) is a non-covalent SARS-CoV-2 MPro inhibitor with a IC50 of 0.04 μM. DNDI-6510 has a potent antiviral activity across SARS-CoV-2 and its variants as well as a weak efficacy to SARS-CoV-1. DNDI-6510 significantly improves drug exposure in metabolically humanized mice model (8HUM) .
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- HY-W197205
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Sirtuin
Histone Acetyltransferase
PEPCK
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Metabolic Disease
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SL010110 is an anti-hyperglycemic agent. SL010110 potently inhibits gluconeogenesis by inhibiting SIRT2, activating p300, and subsequently promoting PEPCK1 degradation. SL010110 downregulates the protein level of PEPCK1 without affecting the gene expressions of PEPCK, glucose-6-phosphatase, and fructose-1,6-bisphosphatase. SL010110 significantly improves glucose homeostasis in type 2 diabetic (T2D) mice model. SL010110 can be used for T2D research .
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- HY-P991609
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MMP
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Cancer
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ABX-MA1 is a humanized IgG2 monoclonal antibody inhibitor targeting MCAM/MUC18. ABX-MA1 significantly decreases homotypic aggregation and heterotypic adhesion to HUVECs, and the formation of experimental lung metastasis. ABX-MA1 potently inhibits tumor growth, angiogenesis, and MMP-2 expression in A375SM/WM2664 xenograft mice model, promising for melanoma research .
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- HY-174247
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PROTACs
PAK
Cadherin
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Cancer
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CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 has potent antimigratory and invasive activity and significantly suppresses the invasion and metastasis of tumor cells in A549-luc lung metastasis mice model . Pink: PAK4 ligand (HY-174822); Blue: CRBN ligase ligand (HY-10984); Black: linker
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- HY-174458
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PROTACs
MDM-2/p53
IKZF Family
Casein Kinase
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Cancer
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MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
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- HY-175231
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5-HT Receptor
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Neurological Disease
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ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41 nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .
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- HY-176239
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PROTACs
PI3K
Akt
Apoptosis
Autophagy
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Cancer
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PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
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- HY-175022
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PROTACs
IRAK
Toll-like Receptor (TLR)
Interleukin Related
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Inflammation/Immunology
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PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research . Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
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- HY-W012481
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Ethylphenylhydantoin; Phenylethyihydantoin; Desmethylmephenytoin
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Drug Metabolite
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Neurological Disease
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Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
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- HY-171804
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FP-020
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MMP
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Inflammation/Immunology
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Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC50: < 10 nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin (HY-108345) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma .
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- HY-N16374
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Antibiotic
Bacterial
Fungal
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Infection
Cancer
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Mazethramycin B (Compound II) is an antitumor antibiotic. Mazethramycin B can be isolated from the Streptomyces thioluteusM ME561-L4. Mazethramycin B has a broad-spectrum antimicrobial activity (such as MICs of 1.56 and 6.25 μg/mL for the bacteria Bacillus subtilis PCI 219 and the fungus Candida pseudotropicalis, resepectively). Mazethramycin B significantly increases survival in L1210 leukemia mice model .
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- HY-178748
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Pyruvate Kinase
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species (ROS)
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Cancer
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PKM2-IN-12 is an orally active PKM2 inhibitor with an IC50 of 10 nM. PKM2-IN-12 inhibits COLO-205 cell proliferation and migration, arrests the cell cycle, and induces apoptosis. PKM2-IN-12 significantly reduces cellular levels of lactate, pyruvate, and ROS. PKM2-IN-12 directly kills cancer cells and restores disrupted gut microbiota balance in mice model. PKM2-IN-12 can be used to study colorectal cancer .
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- HY-P10966A
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IKK
NF-κB
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Inflammation/Immunology
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Tat-IKIP (46-60) TFA is the trifluoroacetic acid of Tat-IKIP (46-60) (HY-P10966). Tat-IKIP (46-60) is a IκB kinase (IKK)-targeting membrane-penetrating peptide. Tat-IKIP (46-60) inhibits IKK activation and NF-κB targeted gene expression by disrupting the IKKβ/NEMO complex. Tat-IKIP (46-60) significantly reduces DSS (HY-116282)-induced acute inflammation in inflammatory bowel disease (IBD) mice model and attenuates Zymosan-induced acute arthritis in acute arthritis model (AAM). Tat-IKIP (46-60) can be used for inflammatory diseases research, such as IBD, pancreatitis and rheumatoid arthritis .
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- HY-P11026
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DOTA-PEG4-TMVP1446
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VEGFR
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Cancer
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DOTA-TMVP1446 is a VEGFR-3 targeting peptide. DOTA-TMVP1446 labeled with 68Ga accurately detectes the status of lymph node metastasis, even in micrometastatic tumors, in the B16-F10 tumor mice model. DOTA-TMVP1446 can be used as a radiotracer for cancer-metastatic sentinel lymph nodes (m-SLN) imaging .
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- HY-N7394
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(3S)-Zuonin A
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AMPK
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Metabolic Disease
Cancer
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Galbacin ((3S)-Zuonin A), the epimer of (-)-Zuonin A (HY-N7394A), is a AMPK activator. Galbacin can be isolated from Myristica fragrans (nutmeg). Galbacin stimulates AMPK enzyme in differentiated C2C12 cells. Galbacin also has anticancer activity, and inhibits the proliferation of lymphocyte and tumor cells. Galbacin prevents weight gain in diet-induced mice model. Galbacin can be used for metabolic syndrome (including obesity and type-2 diabetes) and caners research .
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- HY-174811
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PROTACs
Epigenetic Reader Domain
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
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- HY-175281
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PROTACs
Src
Discoidin Domain Receptor
Bcr-Abl
Apoptosis
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Cancer
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SJ11646 is a Dasatinib (HY-10181)-based LCK PROTAC degrader with a DC50 of 0.00838 pM. SJ11646 has potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples with drastically prolonged suppression of LCK signaling, and induces T-ALL apoptosis. SJ11646 binds to 51 human kinases with a high affinity (particularly ABL1, KIT, and DDR1). SJ11646 has superior antileukemic efficacy in T-ALL mice model. . Pink: LCK ligand (HY-107447); Blue: CRBN ligase ligand (HY-163169); Black: linker (HY-76667)
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- HY-P4650
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Tyrosylhistidine is a dipeptide consisting of tyrosine and histidine (Tyr-His). Tyrosylhistidine is an orally active antihypertensive peptide. Tyrosylhistidine reduces blood pressure in mice in a model of spontaneous hypertension .
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- HY-121007
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Web2170
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Platelet-activating Factor Receptor (PAFR)
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Others
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Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guinea pigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
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- HY-P991634
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CD73
TNF Receptor
Interleukin Related
IFNAR
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Inflammation/Immunology
Cancer
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IBI-325 is a humanized monoclonal antibody inhibitor targeting CD73. IBI-325 completely inhibits CD73 enzymatic activity without hook effect. IBI-325 reverses Adenosine monophosphate (HY-A0181)-mediated immune suppression and significantly inhibits T cell proliferation and cytokines (IL-2, IFN-γ and TNF-α) release. IBI-325 has potent antitumor activities in hPBMC-reconstituted mice model and hCD73 knock-in mice model. IBI-325 can be used for cancer immunotherapy research .
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- HY-177270
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EGFR
Drug Derivative
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Cancer
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CHNQD-01281, a derivative of Brefeldin A (HY-16592), is a EGFR modulator. CHNQD-01281 has strong antiproliferative activities against cancer cells (IC50: 0.079 and 0.081 μM for T24 and J82 cells, respectively). CHNQD-01281 regulates both EGFR/PI3K/AKT and EGFR/ERK pathways and mediates the chemotactic effect of chemokines on immune effector cells. CHNQD-01281 remarkably inhibits tumor growth in T24 xenograft mice model and prolongs the survival time in MB49 allogeneic mice model via inducing infiltration of cytotoxic T cells .
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- HY-171956
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Proteasome
Parasite
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Infection
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Carmaphycin-17 (CP-17) is a selective 20S proteasome inhibitor with an EC50 of 217 ?nM. Carmaphycin-17 has potent antimicrobial activity against Trichomonas vaginalis. Carmaphycin-17 overcomes Metronidazole (HY-B0318) resistance and significantly reduces parasite burden upon topical treatment without any apparent adverse effects in vaginal trichomonad infection mice model. Carmaphycin-17 can be used for sexually transmitted disease like trichomoniasis research .
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- HY-P10992
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PI3K
Akt
mTOR
Caspase
Apoptosis
Bcl-2 Family
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Cancer
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YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research .
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- HY-174339
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Phosphodiesterase (PDE)
Heme Oxygenase (HO)
NF-κB
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Neurological Disease
Inflammation/Immunology
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Neuroprotective agent 12 is an orally active and BBB-penetrable neuroprotective agent. Neuroprotective agent 12 has potent neuroprotective effects with robust anti-oxidation and anti-inflammation. Neuroprotective agent 12 significantly inhibits glutamate- and acrolein-induced cell death, reduces PDE4B expression but increases the HO-1, p-CREB and BDNF levels. Neuroprotective agent 12 exhibits potent neuroprotection in traumatic brain injury (TBI) mice model, promising for TBI and other central nervous system diseases .
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- HY-175014
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PD-1/PD-L1
Biochemical Assay Reagents
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Cancer
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LGT-1 is a PD-L1 ligand. LGT-1 labeled with 18F has an excellent specific uptake in B16-F10 tumor cells, and shows a high tumor uptake but a low liver uptake with good stability in B16-F10 tumor-bearing mice model. LGT-1 can be used as a radiotracer for PET imaging of PD-L1 expression in tumors .
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- HY-174415
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PROTACs
EGFR
Akt
ERK
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Cancer
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ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFR L858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR L858R/T790M/C797S xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
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- HY-165606
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Oct3/4
c-Myc
Apoptosis
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Cancer
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SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133 +/CD44 + cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers .
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- HY-177091
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PIKfyve
Interleukin Related
MHC
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Inflammation/Immunology
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AS2795440 is a PIKfyve inhibitor. AS2795440 selectively inhibits proinflammatory cytokine such as IL-12p40 and IL-6 production and B cell activation without affecting Ca 2+ signaling. AS2795440 significantly reduces joint inflammation and bone loss in adjuvant-induced arthritis (AIA) mice model. AS2795440 can be used for inflammatory and autoimmune diseases like rheumatoid arthritis, psoriasis and inflammatory bowel disease research .
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- HY-P11004
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Bacterial
Antibiotic
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Infection
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A3-APO is an antimicrobial peptide. A3-APO has a significant antimicrobial activity by a dual mode of action with both membrane disintegration and intracellular target inhibition. A3-APO can deactivate bacterial toxins and increase the expression of anti-inflammatory cytokines (such as IL-4 and IL-10), without antimicrobial resistance. A3-APO accelerates burn wounds healing in mice infection model of Acinetobacter baumannii and Staphylococcus aureus .
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- HY-106159
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Reactive Oxygen Species (ROS)
p38 MAPK
JNK
PERK
Ferroptosis
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Cancer
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SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel (HY-B0015) resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model .
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- HY-W795993
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Transmembrane Glycoprotein
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Inflammation/Immunology
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TJU103 is a CD4 inhibitor. TJU103 inhibits autoreactive CD4 + T cells by disrupting the function of the CD4 during activation. TJU103 decreases mononuclear cell infiltration in brain and spinal cord tissue of experimental allergic encephalomyelitis (EAE) mice model. TJU103 downregulates Th1 and Th2 cytokine levels in response to proteolipid protein epitope 139-151 (PLPe) and exhibits inhibitory effects both after the appearance of EAE symptoms and upon rechallenge with Ag. TJU103 can be used for autoimmune diseases like EAE and sclerosis (MS) research .
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- HY-P10988
-
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Apoptosis
MDM-2/p53
Integrin
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Cancer
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LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model .
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- HY-178775
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PI4K
Parasite
MAP4K
PI3K
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Infection
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PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria .
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- HY-P991566
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CTLA-4
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Cancer
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KD6001 is a humanized IgG1κ monoclonal antibody, targeting CTLA4. KD6001 significantly disrupts CTLA-4 interactions with CD80 (IC50: 16 ng/mL) and CD86. KD6001 enhances IL-2 and IFNγ expression in PHA-activated human lymphocytes and exhibits potent antitumor effects. KD6001 effectively inhibits tumor growth in MC38, B16, and Hepa1-6 tumor mice model. KD6001 can be used for cancers research, such as advanced melanoma, hepatocellular carcinoma and liver cancer .
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-
-
- HY-W841438
-
|
|
Amyloid-β
Tau Protein
|
Neurological Disease
|
|
Lithium orotate is an orally active lithium supplement with reduced binding that can bypass amyloid sequestration in AD mice models. Lithium orotate can prevent Aβ plaque deposition and phospho-tau accumulation and reverse AD pathology, neuroinflammatory changes and memory loss in AD mice models and ageing wild-type mice. Lithium orotate can be used for the research of alcoholism and Alzheimer’s disease .
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-
-
- HY-178008
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cancer
|
|
Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC) .
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-
-
- HY-P11018
-
|
|
Peptide-Drug Conjugates (PDCs)
Ephrin Receptor
|
Cancer
|
|
(123B9)2-L2-PTX is an EphA2-agonistic peptide-drug conjugate (PDC). (123B9)2-L2-PTX consists of a dimeric 123B9 (HY-P10579) and Paclitaxel (HY-B0015). (123B9)2-L2-PTX significantly reduces circulating tumor cells and inhibits lung tumor metastasis in breast-cancer-Metastasis mice model. (123B9)2-L2-PTX can be used for cancers research, such as melanomas and ovarian and breast cancers .
|
-
- HY-176225
-
|
|
PROTACs
Src
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
|
-
- HY-174405
-
|
|
PROTACs
Phosphodiesterase (PDE)
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
PROTAC PDE4 degrader-1 (Compound 9m) is a selective and orally active PDE4 PROTAC degrader with a DC50 of 41.98 μM. PROTAC PDE4 degrader-1 potently inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. PROTAC PDE4 degrader-1 significantly alleviates pulmonary inflammation in LPS (HY-D1056)-induced acute lung injury (ALI) mice Model . Pink: PDE4 ligand (HY-174410); Blue: CRBN ligase ligand (HY-10984); Black: linker
|
-
- HY-172350
-
|
|
SARS-CoV
Virus Protease
Interleukin Related
|
Infection
|
|
WEHI-P8 is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC50 of 12 nM and a Kd of 9.0 nM. WEHI-P8 reduces viral load, body weight loss, pulmonary inflammation, immune cell infiltration and pro-inflammatory mediator levels in SARS-CoV-2-infected mice. WEHI-P8 prevents pulmonary hemorrhage, immune cell infiltration, fibrotic remodeling and neuroinflammation, and improves cognitive function in a mouse model of post-acute sequelae of SARS-CoV-2 infection (PASC). WEHI-P8 is applicable for the research of COVID-19 and PASC .
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-
- HY-174315
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
Akt
ERK
|
Cancer
|
|
WZH-17-002 is a WZH-15-125-based ALK PROTAC degrader with a DC50 of 25 nM. WZH-17-002 enhances activities against Lorlatinib (HY-12215)-resistant ALK compound mutations. WZH-17-002 significantly reduces drug resistance in ALK-fusion non-small cell lung cancer (NSCLC) and inhibits tumor growth in EML4-ALK G1202R/L1196 M xenograft mice model . Pink: ALK ligand (HY-174314); Blue: CRBN ligase ligand (HY-14658); Black: linker (HY-174316)
|
-
- HY-176220
-
|
|
AUTACs
Autophagy
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
|
-
- HY-174820
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
Cancer
|
|
AZ'320 is an ATP-competitive necroptosis (EC50 of 4.9 μM) inhibitor and a RIPK1 (pKD of 5.45) inhibitor. AZ'320 inhibits necroptosis by inhibiting RIPK1 phosphorylation. AZ’320 prevents mortality of the mice and rescues temperature and body weight in SIRS mice models. AZ'320 can be used for researches of cancer and inflammation .
|
-
- HY-P991595
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
HB-0017 is a humanized IgG1κ monoclonal antibody inhibitor, targeting IL-17A. HB-0017 inhibits the IL-6 secretion induced by IL-17A with an IC50 of 2.09 nM. HB-0017 significantly decreases ear thickness in Imiquimod (HY-B0180)-induced psoriasis-like mice model and alleviates inflammations in IL-17A-induced arthritis and air pouch mice model. The isotype control for the HB-0017 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-175361
-
|
|
ROR
|
Cancer
|
|
RORγ agonist 2 (Compound 34) is a selective RORγ agonist with an EC50 of 0.03 μM for hRORγ. RORγ agonist 2 significantly inhibits tumors growth in syngeneic MC38 tumor mice model .
|
-
- HY-147720A
-
|
|
γ-secretase
|
Neurological Disease
|
|
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease .
|
-
- HY-100679B
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
(R)-Pirlindole mesylate is selective and reversible a Monoamine oxidase A (MAO-A) inhibitor with an IC50 of 0.43 μM for MAO-A over MAO-B. (R)-Pirlindole mesylate has an antidepressant activity. (R)-Pirlindole mesylate significantly decreases immobility time of the forced swim test and inhibits Reserpine (HY-N0480)-induced palpebral ptosis in behavioural mice models. (R)-Pirlindole mesylate can be used for depression research .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-175305
-
|
|
Parasite
|
Infection
|
|
DMU759 is a Lysyl-tRNA synthetase 1 (KRS1) inhibitor. DMU759 has potent anti-kinetoplastid activity against Trypanosoma cruzi , Trypanosoma brucei and Leishmania donovani. DMU759 significantly reduces parasitemia in acute Chagas disease mice model. DMU759 can be used for parasitic infection like Chagas disease research .
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-
- HY-174330A
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-31 hydrochloride is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 hydrochloride has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 hydrochloride significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
|
-
- HY-174330
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
|
-
- HY-P10966
-
|
|
IKK
NF-κB
|
Inflammation/Immunology
|
|
Tat-IKIP (46-60) is a IκB kinase (IKK)-targeting membrane-penetrating peptide. Tat-IKIP (46-60) inhibits IKK activation and NF-κB targeted gene expression by disrupting the IKKβ/NEMO complex. Tat-IKIP (46-60) significantly reduces DSS (HY-116282)-induced acute inflammation in inflammatory bowel disease (IBD) mice model and attenuates Zymosan-induced acute arthritis in acute arthritis model (AAM). Tat-IKIP (46-60) can be used for inflammatory diseases research, such as IBD, pancreatitis and rheumatoid arthritis .
|
-
- HY-171953
-
|
|
Liposome
|
Others
|
|
THP1 Lipid is an ionizable lipidoid. THP1 Lipid can be used to synthesize lipid nanoparticles (LNPs) for delivering mRNA to muscles with minimal toxicity and editing genes in specific liver tissues in tdTomato transgenic mice model. THP1 Lipid can be used for vaccine delivery and CRISPR/Cas9-mediated gene editing research .
|
-
- HY-P11075
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research .
|
-
- HY-P991587
-
|
|
Orphan GPCR
|
Cancer
|
|
SAR-446523 is a humanized IgG1 monoclonal antibody inhibitor targeting GPRC5D. SAR-446523 significantly induces antibody-dependent cell-mediated cytotoxicity (ADCC). SAR-446523 has potent antitumor activity with improvement of mouse survival in NK humanized NOG huIL15 transgenic mice model bearing MM cells. SAR-446523 can be used for multiple myeloma (MM) research .
|
-
- HY-P11028
-
|
|
CDK
|
Cancer
|
|
M1-20 is a CDK1 inhibitor. M1-20 promotes CDK1 ubiquitination by CUL4-DDB1-DCAF1 complexes and degradation through the proteasome pathway. M1-20 abolishes the formation of CDK1/CCNB1 complexes. M1-20 has significant anticancer activity of spontaneous breast cancer in FVB/N MMTV-PyVT mice model .
|
-
- HY-177268
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
PARP
Caspase
Akt
|
Cancer
|
|
CHNQD-01426 (Compound 4a) is an anticancer agent. CHNQD-01426 has cytotoxic activities against cancer cells. CHNQD-01426 significantly inhibits hepatocellular carcinoma cells proliferation via arresting S and G2/M phase cell cycle and induces apoptosis by inducing ROS production and elevating apoptosis-related proteins expression. CHNQD-01426 potently inhibits tumor growth in HepG2 xenograft mice model .
|
-
- HY-175201
-
|
|
LPL Receptor
STAT
|
Cancer
|
|
pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
|
-
- HY-N16371
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid (Compound MC-1), an isocoumarin, is a metabolite of Cytogenin (HY-19606). 6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid has anti-angiogenic activity in S-180 implanted dorsal air sac mice model. 6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid also modifies collagen-induced arthritis. 6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid can be used for cancers and inflammatory diseases research .
|
-
- HY-P10977
-
|
|
Sodium Channel
RIP kinase
|
Neurological Disease
|
|
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
|
-
- HY-175206
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp-IN-30 (Compound 13) is a P-glycoprotein (P-gp) inhibitor by targeting YB-1. P-gp-IN-30 significantly enhances sensitivity to Paclitaxel by reducing total YB-1 and nucleus YB-1 protein expression, inhibiting the expression and function of downstream P-gp, further suppressing the efflux rate of Paclitaxel. P-gp-IN-30 potently inhibits tumor growth in A549/Taxol xenografts mice model with combination of Paclitaxel (HY-B0015). P-gp-IN-30 can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-172099
-
-
- HY-N1149
-
|
(-)-Tilifodiolide
|
Others
|
Others
|
|
Tilifodiolide ((-)-Tilifodiolide) is a lactone, which can be isolated from the roots of Salvia tiliaefolia. Tilifodiolide has anti-inflammatory activity in mice model .
|
-
- HY-163346
-
-
- HY-106471
-
|
Propyldazine
|
Others
|
Cardiovascular Disease
|
|
Pildralazine (Propyldazine) is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally active, has no significant carcinogenicity in mice model .
|
-
- HY-122323
-
|
Leucylarginine
|
Amino Acid Derivatives
|
Others
|
|
L-Leucyl-L-arginine (Leucylarginine) is a compound that inhibits the analgesic effect of systemically administered L-arginine in a carrageenan-induced hyperalgesia model in mice when administered intracerebroventricularly.
|
-
- HY-161926
-
|
|
PPAR
|
Metabolic Disease
|
|
YGT-31 is a modulator for PPARγ with an IC50 of 1.72 μM, and a Ki of 0.62 μM. YGT-31 reduces blood glucose levels and improves insulin resistance in db/db mice type 2 diabetes models, through inhibition of CDK5-mediated PPARγ-Ser273 phosphorylation. YGT-31 exhibits anti-hepatic steatosis effect in mice non-alcoholic fatty liver disease (NAFLD) model .
|
-
- HY-P10312
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models .
|
-
- HY-118537
-
|
|
Parasite
|
Infection
|
|
ICI 56780 is an antimalarial agent, that exhibits etiological prevention and blood schizonticidal activity in rodent malaria models. ICI 56780 develops parasite resistance in P. berghei infected mice .
|
-
- HY-121671
-
|
|
RAR/RXR
|
Neurological Disease
|
|
TBTC is a selective agonist with the activity of improving behavioral deficits in Alzheimer's disease model mice. TBTC can effectively activate the heterodimerization of RXRα with LXRα or PPARγ. TBTC stimulates the expression of apoE, ABCA1, and ABCG1 genes and reduces Aβ content in cells and animal models .
|
-
- HY-126835
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
A 924 is an amino acid derivative-based, orally active antitumor agent. A 924 is effective in inhibiting ascites tumors in rat models by intraperitoneal injection or oral administration. The LD50 of A 924 in mice is >1.5 g/kg and >4.5 g/kg by intraperitoneal injection or oral administration, respectively. A 924 does not cause teratogenicity or adverse reactions in normal or pregnant mice .
|
-
- HY-114527
-
|
|
Apoptosis
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
|
-
- HY-168214
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
|
-
- HY-121365
-
|
|
Bacterial
|
Infection
|
|
Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
|
-
- HY-15041
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
NVP-SAA164 is an orally active nonpeptide kinin B1 receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .
|
-
- HY-W012481R
-
|
Ethylphenylhydantoin (Standard); Phenylethyihydantoin (Standard); Desmethylmephenytoin (Standard)
|
Drug Metabolite
Reference Standards
|
Neurological Disease
|
|
Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
|
-
- HY-169928
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 14 (compound S35) is an orally active WRN inhibitor with anticancer activity. WRN inhibitor 14 results in tumor growth inhibition in the SW48 xenograft model in BALB/c nude mice .
|
-
- HY-113354R
-
|
|
Reference Standards
Endogenous Metabolite
|
Neurological Disease
|
|
Anserine (Standard) is the analytical standard of Anserine. This product is intended for research and analytical applications. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
|
-
- HY-110303
-
|
XAC dihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-167655
-
|
|
Androgen Receptor
|
Others
|
|
KF-19418 is a hair follicle stimulator with hair growth promoting activity. KF-19418 stimulates proliferation of cultured hair bulb cells from newborn mice. KF-19418 accelerates hair regrowth in hair-clipped mouse alopecia model following topical application. KF-19418 can be used for the research of alopecia .
|
-
- HY-182782
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
Analgesic agent-4 is an adenosine A3AR ligand with analgesic/antinociceptive activity. Analgesic agent-4 inhibits writhing responses in mice and exhibits dose-dependent activity in the acetic acid (HY-Y0319)-induced mouse writhing model. Analgesic agent-4 can be used in the research of pain-related diseases .
|
-
- HY-P991966
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse EGFR Antibody (7A7) ia an anti-mouse EGFR monoclonal antibody proposed to be the mouse equivalent of cetuximab. Anti-Human/Mouse EGFR Antibody (7A7) fails to induce tumor regression in the HPV38 tumor model where EGFR is not expressed in mice. Anti-Human/Mouse EGFR Antibody (7A7) can be used in EGFR-expressing HPV38 tumor-related studies .
|
-
- HY-W783351
-
|
Coppersensor 790 acetoxymethyl ester
|
Fluorescent Dye
|
Metabolic Disease
|
|
CS790AM (Coppersensor 790 acetoxymethyl ester) is a cell-permeable, Cu +-targeted near-infrared fluorescent probe (λabs=760 nm, λem=790 nm) applicable to live cells. CS790AM can cross lipophilic cell membranes, and is converted into negatively charged CS790 under the action of intracellular esterases to be retained, thus enabling highly sensitive, reversible "turn-on" detection of labile Cu + pools in live cells and mice. CS790AM possesses excellent biocompatibility and selectivity, avoids interference from other metal ions, shows no obvious toxicity, and can be rapidly cleared. CS790AM allows long-term longitudinal monitoring of individual mice, visualizes copper levels in internal organs and isolated livers, and effectively evaluates abnormal copper accumulation in Wilson's disease models (Atp7b -/-) as well as dynamic changes after chelator treatment. CS790AM can be used for research on Wilson's disease and related copper metabolic disorders .
|
-
- HY-P991881
-
|
|
TGF-β Receptor
Hepcidin
Ferroportin
|
Cardiovascular Disease
|
|
KY1070 is a fully human anti-BMP6 antibody with a Kd of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease [1] [2].
|
-
- HY-110268
-
|
|
CXCR
|
Inflammation/Immunology
|
|
NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-182648
-
|
|
|
Neurological Disease
|
|
K811 is an orally active ASK1 inhibitor with an IC50 of 6 nM. K811 inhibits glial cell activation in the lumbar spinal cord of SOD1 G93A transgenic mice. K811 extends the survival of SOD1 G93A transgenic mice, a mouse model of amyotrophic lateral sclerosis. K811 can be used in studies related to amyotrophic lateral sclerosis .
|
-
- HY-101139B
-
|
XAC trihydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
|
Xanthine amine congener trihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
|
-
- HY-110262
-
|
|
MAP3K
p38 MAPK
|
Inflammation/Immunology
|
|
MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation .
|
-
- HY-137440A
-
|
TAK-994
|
Orexin Receptor (OX Receptor)
ERK
|
Neurological Disease
|
|
Firazorexton hydrate (TAK-994) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton hydrate can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice .
|
-
- HY-137440
-
|
TAK-994 free base
|
Orexin Receptor (OX Receptor)
ERK
|
Neurological Disease
|
|
Firazorexton (TAK-994 free base) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton (TAK-994 free base) can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice .
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-135042
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model .
|
-
- HY-109120
-
|
A4250
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
|
Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
|
-
- HY-14364
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
|
-
- HY-173517
-
|
|
Na+/H+ Exchanger (NHE)
|
Neurological Disease
|
|
NHE-1-IN-2 (compound 7g) is a potent NHE-1 inhibitor with an IC50 of 0.78 μM. NHE-1-IN-2 alleviates left ventricular systolic dysfunction in mice model of heart failure .
|
-
- HY-12192
-
|
|
Histamine Receptor
|
Metabolic Disease
|
|
A-423579 is an orally active non-imidazole histamine H3 receptor antagonist. A-423579 exhibits high affinity and good selectivity for human and rat H3 receptors, and possesses both antagonistic and inverse agonistic activities. A-423579 can effectively reduce body weight in obese rodents, with concomitant decreases in fat content, plasma leptin levels, and triglycerides. A-423579 possesses anti-obesity activity and can be used in the research of obesity and related metabolic disorders .
|
-
- HY-P11005
-
|
|
Dynamin
ATP Synthase
|
Neurological Disease
|
|
P259 is a Drp1-Mff inhibitor. P259 distinguishes physiological from pathological fission by specifically inhibiting Drp1-Mff interaction. P259 elongates cell mitochondria and disrupts mitochondrial function and motility. P259 reduces ATP levels and alters mitochondrial structure in the brain, resulting in behavioral deficits in wild-type mice and a short lifespan in Huntington's disease (HD) mice model .
|
-
- HY-161618
-
|
|
JAK
EGFR
PI3K
IGF-1R
GSK-3
|
Inflammation/Immunology
Endocrinology
|
|
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
|
-
- HY-162477
-
|
|
Cathepsin
Apoptosis
|
Cancer
|
|
TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
|
-
- HY-13513
-
|
SLC-0111
|
Carbonic Anhydrase
|
Cancer
|
|
U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model .
|
-
- HY-181996
-
|
|
Btk
Caspase
Apoptosis
PARP
|
Cancer
|
|
BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies .
|
-
- HY-149401
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
|
-
- HY-158093
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages .
|
-
- HY-100827
-
|
LF22-0542
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
|
-
- HY-147529
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice .
|
-
- HY-180323
-
|
|
RAR/RXR
|
Inflammation/Immunology
|
|
ER-38925 is a retinoid agonist with selevtivity to retinoic acid receptor subtype α (RAR-α). ER-38925 prolongs the lifespan of the recipient mice dose-dependently. ER-38925 potently inhibits alloantigenstimulated donor T lymphocyte prolifertion in vitro. ER-38925 can prevent the development of antiallogeneic cytotoxic T lymphocyte response in mice. ER-38925 inhibits serum anti-DNA autoantibody production in mouse model of human chronic GVHD .
|
-
- HY-N3312S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Infection
|
|
Matairesinol-d6 is the deuterium labeled Matairesinol. Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-114611
-
|
|
IRE1
|
Metabolic Disease
|
|
BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress .
|
-
- HY-110192
-
ML 297
1 Publications Verification
VU 0456810; CID 56642816
|
Potassium Channel
|
Neurological Disease
|
|
ML 297 (VU 0456810) is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM. ML 297 can cross the blood-brain barrier with brain-to-plasma ratio of 0.2 in mice model (i.p.). ML 297 is potential for the treatment of epilepsy .
|
-
- HY-105365
-
|
|
Calcium Channel
|
Neurological Disease
|
|
PD 175069 is a potent and selective N-type calcium channel antagonist with an IC50 of 0.32 μM. PD 175069 is efficacious in an audiogenic seizure model using DBA/2 mice. PD 175069 can be used for research on neurological conditions such as neuropathic pain and stroke .
|
-
- HY-119805
-
|
|
Others
|
Inflammation/Immunology
|
|
YM 13650 is an orally active anti-nephritic agent. YM 13650 exhibits dose-dependent preventive and therapeutic effects in both the rat immune complex nephritis model and the mouse spontaneous lupus nephritis model. YM 13650 can inhibit the increase in urinary protein, improve serum cholesterol and urea nitrogen levels, alleviate renal pathological damage, and prolong the survival time of mice. YM 13650 can be used in the research of nephritic diseases .
|
-
- HY-105063
-
|
|
HSP
|
Metabolic Disease
Inflammation/Immunology
|
|
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes .
|
-
- HY-P99216
-
|
PF-04360365; RN 1219
|
Amyloid-β
|
Neurological Disease
|
|
Ponezumab (PF-04360365; RN 1219) is a humanized anti-amyloid-β (Amyloid-β) IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves the performance of mice in various learning and memory models. Ponezumab is applicable to the research of Alzheimer's disease .
|
-
- HY-144361
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
|
-
- HY-147014
-
|
|
CMV
Orthopoxvirus
|
Infection
|
|
Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guinea pig cytomegalovirus (GPCMV) infection and decreases viral replication in guinea pig model .
|
-
- HY-N3312R
-
|
|
Reference Standards
Endogenous Metabolite
|
Infection
|
|
Matairesinol (Standard) is the analytical standard of Matairesinol. This product is intended for research and analytical applications. Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-153306
-
|
RLY-2608
|
PI3K
|
Cancer
|
|
Zovegalisib (RLY-2608) is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. Zovegalisib inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
|
-
- HY-170933
-
|
|
SGK
|
Cancer
|
|
SGK1-IN-6 (compound 12f) is a potent SGK1 inhibitor with an IC50 of 0.39 μM. SGK1-IN-6 suppresses tumor growth in the PC3 xenograft model in BALB/c nude mice without inducing any observable toxicity .
|
-
- HY-168021
-
|
|
Monoamine Oxidase
Serotonin Transporter
|
Neurological Disease
|
MAO-A/SERT-IN-1 is an inhibitor of MAO-A/serotonin transporter (SERT). MAO-A/SERT-IN-1 can reduce SERT-mediated reuptake of 5-HT and has neuroprotective effects in cell inhibition models. MAO-A/SERT-IN-1 can improve depressive behavior in zebrafish and mice .
|
-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-149429
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) .
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-172105
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-NASH agent 2 (compound 21) is an inhibitor of de novo adipogenesis activity and α-SMA gene expression. Anti-NASH agent 2 improves hepatic steatosis, edema, inflammatory infiltrates, and liver fibrosis in NASH mouse models .
|
-
- HY-178214
-
|
|
Ser/Thr Kinase
Lipoxygenase
|
Inflammation/Immunology
|
|
CSBP ligand 1 (Compound 36) is a ligand of CSBP, with an IC50 of 0.08 μM for CSBP binding. CSBP ligand 1 can inhibit the production of TNF in mice treated with LPS (HY-D1056). CSBP ligand 1 has no significant inhibitory activity against PGHS-1 (IC50: 16 μM) and 5-LO (IC50: 60 μM). CSBP ligand 1 can be used in the research of inflammation-related diseases .
|
-
- HY-176957
-
|
|
Wee1
|
Cancer
|
|
PKMYT1-IN-11 (Example 1) is a PKMYT1 inhibitor with an IC50 of 4.49 nM. PKMYT1-IN-11 inhibits the proliferation of HCC1569 cells. When combined with Gemcitabine (HY-17026), PKMYT1-IN-11 shows a significant anti-tumor effect in the OVCAR3 xenograft mouse model. PKMYT1-IN-11 can be used for the study of various cancers such as breast cancer and ovarian cancer .
|
-
- HY-D2279
-
|
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively .
|
-
- HY-158311
-
|
|
RANKL/RANK
p38 MAPK
NF-κB
|
Endocrinology
|
|
Anti-osteoporosis agent-8 (Compound 4aa) is an inhibitor for RANKL, which inhibits RANKL-induced osteoclastogenesis and osteoclast differentiation (IC50 is 2.41 μM) in cells RAW264.7. Anti-osteoporosis agent-8 ameliorates bone loss in an ovariectomized (OVX) mice model .
|
-
- HY-120291
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ASP9436 is an orally active and blood-brain barrier permeable PDE10A inhibitor with an IC50 of 8 nM against human PDE10A. ASP9436 attenuates locomotor activity in mouse hyperactivity models and ameliorates visual recognition memory impairment in neonatal mice. ASP9436 is applicable to research related to schizophrenia .
|
-
- HY-174325
-
|
|
Parasite
|
Infection
Inflammation/Immunology
|
|
Antimalarial agent 50 is an antiplasmodial compound. Antimalarial agent 50 has an effect against Plasmodium berghei induced malaria infection in mice model. Antimalarial agent 50 can regulate oxidative stress and significantly reduce the levels of inflammatory factors. Antimalarial agent 50 can be used for the research of the malaria.
|
-
- HY-129442
-
|
X 910279; HMR-279; FK-779
|
Drug Derivative
|
Inflammation/Immunology
|
|
MNA 279 (X 910279) is an orally active, immunosuppressive malononitrilamide and A 771726 derivative. MNA 279 suppresses IgM and IgG antibody production. MNA 279 prevents the development of systemic lupus erythematosus (SLE)-like disease in mice. MNA 279 prolongs skin xenograft survival in a mouse-to-rat model .
|
-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-13554
-
|
|
Antibiotic
|
Cancer
|
|
Annamycin is an anthracycline antibiotic with antitumor activity. Annamycin interacts with topoisomerase II, induces double-strand DNA breaks, triggers cell death, and exerts cytotoxic effects. In mice, Annamycin inhibits the growth of advanced subcutaneous melanoma and subcutaneous squamous cell carcinoma, and prolongs the survival of mice with subcutaneous reticulosarcoma and in lung cancer lung metastasis models. Annamycin can be used in research related to melanoma, reticulum cell sarcoma, lung cancer, non-small cell lung cancer, small cell lung cancer .
|
-
- HY-P991542
-
|
|
CD19
|
Cancer
|
|
GBR-401 is a humanized anti-CD19 monoclonal antibody with high affinity for FcγRIIIa. GBR-401 exerts a potent in vitro and in vivo cytotoxic activity against various B-cell malignancies. GBR-401 induces cell death by antibody dependent cellular cytotoxicity (ADCC) and direct killing effect. GBR-401 demonstrates potent activity of depleting malignant B cells and prolongs mice survival in multiple xenograft severe combined immunodeficiency (SCID) mice models .
|
-
- HY-175430
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-26 (Compound 18) is a TNF-α inhibitor with an IC50 of 0.10 μM for CSBP ligands. TNF-α-IN-26 inhibits LPS (HY-D1056)-stimulated TNF production in mice model. TNF-α-IN-26 can be used for inflammatory diseases research .
|
-
- HY-109120S
-
-
- HY-164320
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-175643
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-58 is a COX-2 inhibitor. COX-2-IN-58 exhibits remarkable anti-inflammatory activity in Carrageenan (HY-125474)-induced paw edema model of Balb/C mice. COX-2-IN-58 can be used for the research of inflammation .
|
-
- HY-109120R
-
|
A4250 (Standard)
|
Apical Sodium-Dependent Bile Acid Transporter
Reference Standards
|
Metabolic Disease
|
|
Odevixibat (Standard) is the analytical standard of Odevixibat. This product is intended for research and analytical applications. Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
|
-
- HY-147720
-
|
|
γ-secretase
|
Neurological Disease
|
|
γ-Secretase modulator 11 (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
|
-
- HY-169104
-
|
|
Bacterial
|
Infection
|
|
InhA-IN-8 (compound 6c) is an orally active inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase). InhA-IN-8 has good inhibitory activity against Mtb UalRv (MIC = 0.5-1 μg/mL). InhA-IN-8 can be used in research on acute tuberculosis model mice .
|
-
- HY-153834
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-167741
-
|
|
nAChR
|
Cardiovascular Disease
Neurological Disease
|
|
Chlorisondamine is a nicotinic antagonist that acts as a ganglionic blocker and has been utilized to evaluate the neurogenic contributions to blood pressure and sympathetic vasomotor tone in animal models. Chlorisondamine has demonstrated antihypertensive properties, primarily being assessed through its effects on blood pressure, cardiac output, and heart rate in various experimental settings, particularly in mice.
|
-
- HY-19606
-
|
Antibiotic MI 43-37F11
|
Interleukin Related
NO Synthase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cytogenin (Antibiotic MI 43-37F11) is an orally active antineoplastic antibiotic. Cytogenin regulates the inflammatory cytokine, reduces the levels of iNOS, NO and IL-6 in mouse macrophages, and exhibits antidiabetic efficacy in mice. Cytogenin inhibits growth of Ehrlich ascites tumor in mouse model .
|
-
- HY-153834A
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
|
-
- HY-170773
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-9 (Compound M1) is a specific Mtb inhibitor that inhibits MtbFadD32 and MtbFadD28 activity. Mtb-IN-9 curtails the Mtb survival in infected macrophages and reduces Mtb burden and tubercular granulomas in a chronic infection model of BALB/c mice. Mtb-IN-9 is promising for research of tuberculosis .
|
-
- HY-103327
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-128850R
-
|
N-Acetylmannosamine (Standard); ManNAc (Standard)
|
Reference Standards
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
N-Acetyl-D-mannosamine (Standard) is an analytical standard for N-Acetyl-D-mannosamine. This product is intended for research and analytical applications. N-Acetyl-D-mannosamine (ManNAc) is an orally active sialic acid (Sialic Acid) precursor that can prevent hypertension by increasing sialylation of IgG and has potential for use in cardiovascular disease research. N-Acetyl-D-mannosamine activates hypocretin (HCRT) gene expression and alters
|
-
- HY-128850
-
|
N-Acetylmannosamine; ManNAc
|
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
|
|
N-Acetyl-D-mannosamine (ManNAc) is an oral active sialic acid precursor that can prevent hypertension by increasing sialylation of IgG, making it a promising candidate for cardiovascular disease research. Additionally, N-Acetyl-D-mannosamine can activate hypocretin (HCRT) gene expression in orexin neurons and improve neurodegeneration caused by aging, offering potential avenues for research in neurological disorders .
|
-
- HY-172456
-
|
|
Bacterial
|
Infection
|
|
JSF-4898 is an orally active inhibitor of the MenG enzyme in Mycobacterium tuberculosis. JSF-4898 has MIC of 0.78 μM against Mycobacterium tuberculosis H37Rv. JSF-4898 can enhance the efficacy of Rifampicin (HY-B0272) in a subacute model of Mycobacterium tuberculosis infection in mice .
|
-
- HY-143420
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model .
|
-
- HY-109120S1
-
-
- HY-161458
-
|
|
GSK-3
Tau Protein
|
Neurological Disease
|
|
GSK-3β inhibitor 16 (compound 7c) is a GSK-3β inhibitor with the IC50 of 4.68 nM. GSK-3β inhibitor 16 decreases Tau hyperphosphorylated aggregate and alleviates cognitive impairments in the Scopolamin (HY-N0296)-induced model in mice .
|
-
- HY-159088
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
|
-
- HY-N11872
-
|
|
Others
|
Neurological Disease
|
|
Suffruticosol A is a neuroprotective agent that restores scopolamine-induced cellular neurodegenerative damage. Suffruticosol A ameliorates hippocampal cholinergic deficits and partially enhances BDNF signaling. Suffruticosol A has neuromodulatory effects in a Scopolamine (HY-N0296)-induced model, restoring memory and cognitive performance in mice. Suffruticosol A can be isolated from seeds of P. lactiflora .
|
-
- HY-113354
-
|
|
Endogenous Metabolite
|
Neurological Disease
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Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine has blood-brain barrier permeability, and improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-66005
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- HY-143237
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Phosphodiesterase (PDE)
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Others
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ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research .
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- HY-159910
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Mitochondrial Metabolism
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Cancer
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LH1513 is a dioxalate derivative of l-lysine (HY-N0469) that inhibits CaOx crystallization with better activity than citrate and pyruvate. LH1513 has potential preventive activity in hyperoxaluria models and effectively prevents urinary CaOx crystal formation in Agxt knockout mice. AGXT-1 is a mitochondrial protein involved in metabolism .
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- HY-168567
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RIP kinase
NF-κB
p38 MAPK
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Inflammation/Immunology
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RIPK2-IN-6 (Compound 15a) is an inhibitor for RIPK, that inhibits the phosphorylation of RIPK2, and thus inhibits the NF-κB and MAPK signaling pathways. RIPK2-IN-6 exhibits anti-inflammatory and anti-fibrotic activities in Dextran sodium sulfate (HY-116282C)-induced mice colitis models .
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- HY-P10580A
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Tie
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
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- HY-P11060
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Adpgk peptide
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MHC
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Cancer
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MC38 SLP Adpgk (Adpgk peptide) is an H-2 K b-restricted colorectal cancer neoantigen peptide. MC38 SLP Adpgk is formulated into PCNP nanocomplexes together with CpG ODN. PCNP vaccines significantly enhance the co-delivery efficiency of neoantigens and adjuvants to lymphoid organs, and activate cytotoxic T cells. PCNP vaccines not only protect mice from MC-38 colorectal tumor invasion, but also exhibit anti-tumor efficacy in established colorectal tumor models and significantly prolong the survival of tumor-bearing mice .
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- HY-N4110
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Cytochrome P450
NF-κB
Interleukin Related
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Friedelin is derived from the leaves of Maytenus ilicifolia (Mart). Friedelin is an orally active non-competitive inhibitor of CYP3A4, with IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin can be used in research related to inflammation, neurological diseases, and metabolic disorders .
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- HY-W424839
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DTBP
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Heme Oxygenase (HO)
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Cardiovascular Disease
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Probucol dithiobisphenol (DTBP) is the derivative of Probucol (HY-B0388). Probucol dithiobisphenol induces the production of heme oxygenase 1 (HO-1), and exhibits antioxidant activity. Probucol dithiobisphenol inhibits atherosclerotic lesions in Apoe −/− mice aorta, promotes re-endothelialization of aorta and inhibits restenosis in rabbit arterial injury models. Probucol dithiobisphenol is orally active .
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- HY-W674149
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Microtubule/Tubulin
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Cancer
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ABI-274 is a tubulin and colchicine binding site inhibitor. ABI-274 significantly promotes cancer cell apoptosis in vitro when combined with vemurafenib (HY-12057). ABI-274 exhibits potent synergistic efficacy in the vemurafenib-resistant xenograft model in nude mice. ABI-274 can be studied in research on melanoma .
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- HY-165571
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Carboxypeptidase
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Neurological Disease
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E2072 is a selective, orally active competitive inhibitor of glutamate carboxypeptidase II (GCPII) with a Ki of 10 nM. E2072 alleviates established thermal hyperalgesia in a rat model of chronic constriction injury. E2072 prevents oxaliplatin-induced reductions in nerve conduction velocity and amplitude in mice. E2072 is applicable to research related to neuropathic pain and neuropathy .
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- HY-N0088
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Acetovanillone
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NADPH Oxidase
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Metabolic Disease
Inflammation/Immunology
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Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
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- HY-117370
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AZ1
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Deubiquitinase
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Cancer
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USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model .
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- HY-156618
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ABSK011
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FGFR
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Cancer
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Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .
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- HY-158812
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Drug Derivative
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Metabolic Disease
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Eicosapentaenoyl-L-carnitine chloride is a long-chain acylcarnitine composed of Eicosapentaenoic Acid (HY-B0660) and L-Carnitine (HY-B0399). The levels of Eicosapentaenoyl-L-carnitine chloride are increased in the eyes of mice fed a diet high in n-3/n-6 polyunsaturated fatty acids (PUFAs) in a mouse model of myopia induced by out-of-focus lenses .
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- HY-176266
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Mitochondrial Metabolism
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Neurological Disease
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KIT-13 is an orally active plasmalogen derivative to inhibit neuroinflammation and mitochondrial DNA leakage associated with Mecp2 deficiency. KIT-13 significantly reduce neurological symptoms and improves the life span of the Rett Syndrome (RTT) model mice. KIT-13 can be used for the study of RTT and other neuroinflammation-related diseases.
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- HY-117924
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Autophagy enhancer-67
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Autophagy
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Neurological Disease
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AUTEN-67 (Autophagy enhancer-67) is an orally active autophagy enhancer and MTMR14 inhibitor. AUTEN-67 has anti-aging and neuroprotective effects. AUTEN-67 protects neurons from stress-induced cell death. AUTEN-67 also restores nesting behavior in a mice model of Alzheimer disease .
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- HY-W012481S
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Ethylphenylhydantoin-d5; Phenylethyihydantoin-d5; Desmethylmephenytoin-d5
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Isotope-Labeled Compounds
Drug Metabolite
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Neurological Disease
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Nirvanol-d5 (Ethylphenylhydantoin-d5) is deuterium labeled Nirvanol (HY-W012481) . Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
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- HY-185585
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Drug Intermediate
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Cancer
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JNJ-27548547, Mitomycin C (HY-13316) prodrug, is a Mitomycin C and lipophilic group conjugate. JNJ-27548547 undergoes thiolytic cleavage of its dithiobenzyl linker in the presence of reducing agents to release active substance Mitomycin C. JNJ-27548547 is formulated into pegylated liposomes (PL-MLP) with high antitumor activity in mice models .
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- HY-161425
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Apoptosis
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Cancer
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Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
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- HY-P11592
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Bacterial
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Infection
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KIKIKPWWWPKIKIK-NH2 is a β-turn antimicrobial peptide. KIKIKPWWWPKIKIK-NH2 can inhibit bacterial biofilm formation and bind to lipopolysaccharid. KIKIKPWWWPKIKIK-NH2 shows wound-healing ability in mice bacteria-infected full-thickness wound models. KIKIKPWWWPKIKIK-NH2 can be used for the research of bacterial infection .
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- HY-113354S
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Endogenous Metabolite
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Neurological Disease
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Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-103089
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5-HT Receptor
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Neurological Disease
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LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression .
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- HY-146054
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CXCR
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Inflammation/Immunology
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CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model .
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- HY-150191
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Lipoxygenase
Acetyl-CoA Carboxylase
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Metabolic Disease
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IMA-1 is an inhibitor that inhibits the interaction between arachidonic acid 12-lipoxygenase (ALOX12) and acetyl-CoA carboxylase 1 (ACC1). IMA-1 significantly blocks the progression of diet-induced non-alcoholic steatohepatitis (NASH) in male mice and crab-eating monkeys, and does not cause hyperlipidemia. IMA-1 can be used for the study of NASH .
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- HY-160887
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5-HT Receptor
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Neurological Disease
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FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
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- HY-P11232
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Toll-like Receptor (TLR)
Bacterial
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Infection
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NAB815 is a specific inhibitor of the Stx2a (Kd = 0.01 μM)/TLR4 interaction. NAB815 inhibits the neutrophil/Stx2a interaction (IC50 = 0.057 μg/mL). NAB815 inhibits the formation of Stx2-containing extracellular vesicles (EVs) produced by leukocytes and platelets and reduces their toxic effects in cellular (Vero cells) and animal models (CD-1 mice). NAB815 reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice. NAB815 is useful in the study of hemolytic uremic syndrome (HUS) .
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- HY-P99148
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TNF Receptor
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Metabolic Disease
Inflammation/Immunology
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Anti-Mouse TNF alpha Antibody (TN3-19.12) is an anti-mouse TNF alpha IgG antibody inhibitor derived from host Armenian Hamster. Anti-Mouse TNF alpha Antibody (TN3-19.12) neutralizes cytotoxic activity in supernatants obtained from LNC-8 cells. Anti-Mouse TNF alpha Antibody (TN3-19.12) reduces the symptoms and severity of EAE (experimental allergic encephalomyelitis) in LNC-8 cells xenograft mice models. Anti-Mouse TNF alpha Antibody (TN3-19.12) prevents diabetes in NOD mice. Anti-Mouse TNF alpha Antibody (TN3-19.12) shows apparent radiosensitizing effect in CD2F1 mice .
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- HY-126850
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EGFR
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Cancer
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4-Epidoxycycline is a liver metabolite of the antibiotic doxycycline (doxycycline, HY-N0565) and doesn't have antibiotic properties in mice. 4-Epidoxycycline’s ability to regulate HER2 gene expression in vitro and in live mouse models is similar to that of doxycycline, and it shows comparable high efficacy in tumor tissues, achieving over 95% tumor regression rates .
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- HY-158374
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IRAK
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Inflammation/Immunology
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BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
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- HY-110190
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ML396
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mGluR
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Neurological Disease
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VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice .
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- HY-156109
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PDHK
Mitochondrial Metabolism
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Cancer
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PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
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- HY-129133
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Drug Isomer
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Others
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cis-Miyabenol C is an isomer of the resveratrol trimer Miyabenol C, which can be isolated from grape herbs. Miyabenol C is an inhibitor of β-amyloid (Aβ) and amyloid β precursor protein (APP) in Alzheimer's disease model mice, and inhibit β-secretase activity without changing the protein level of β-secretase BACE1 .
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- HY-126477
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NNK
2 Publications Verification
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Endogenous Metabolite
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Cancer
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NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
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- HY-165421
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Mps1
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Cancer
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Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
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- HY-175668
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Potassium Channel
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Neurological Disease
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IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy .
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- HY-182367
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GPR39
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Neurological Disease
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TMN-OMe is a blood-brain barrier-permeable GPR39 agonist and a radiotracer for positron emission tomography (PET). TMN-OMe activates GPR39 by recruiting β-arrestin, exhibits highly selective binding ability in the mouse brain, and enables quantitative analysis of GPR39 at the in vivo level. TMN-OMe shows specific uptake in GPR39 knockout mice, Alzheimer's disease model (APP/PS1) mice, and blocking experiments. TMN-OMe facilitates in-depth exploration of changes in GPR39-related mechanisms in neurological diseases and is widely used in Alzheimer's disease research .
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- HY-119468
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Dopamine Transporter
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Neurological Disease
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Medifoxamine is an orally active monoamine reuptake inhibitor and antidepressant. Medifoxamine preferentially inhibits presynaptic dopamine reuptake. Medifoxamine acts as an intraocular pressure-lowering agent to reduce intraocular pressure, and also functions as a miotic agent to decrease pupil diameter. Medifoxamine exhibits characteristic properties of antidepressant compounds, including preventing hypothermia induced by Reserpine (HY-N0480) or Apomorphine (HY-12723), potentiating the toxic effects of Yohimbine (HY-N0127) in mice, and reducing immobility behavior in mice and rats in the "behavioral despair" model. Medifoxamine has no anticholinergic activity. Medifoxamine can be used in research related to depression .
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- HY-15815
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Epigenetic Reader Domain
Apoptosis
CDK
HIV
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Cancer
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Bromosporine, a chemical probe, is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-Fluorouracil (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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- HY-178999
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Drug Derivative
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Cancer
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Carnosol analog 1 (Compound 10) is a derivative of carnosol. Carnosol analog 1 attenuates myotube atrophy (67.08% reversal) and adipocyte lipolysis in C26 tumor-conditioned models. Carnosol analog 1 alleviates cachexia-related weight loss without altering tumor progression in C26 tumor-bearing mice. Carnosol analog 1 can be used for the study of cancer cachexia .
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- HY-N6967
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(-)-α-Bisabolol
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Environmental Pollutants
Apoptosis
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Neurological Disease
Inflammation/Immunology
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Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
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- HY-161373
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PI3K
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Cancer
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PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
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- HY-153903
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Biochemical Assay Reagents
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Others
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RASP-IN-1 (compound A) is a lipophili ccompound used for macular degeneration inhibition. RASP-IN-1 is biologically active in the retina of the rabbit's eye. Thirty minutes after IP treatment with 14C-RASP-IN-1 (10 mg/kg),the Cmax amount of 14C-RASP-IN-1 in the posterior eye cup is 14.36 μg/g in mice model .
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- HY-162646
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Thrombin
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Cardiovascular Disease
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FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg) .
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- HY-155032
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P-glycoprotein
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Cancer
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P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity,and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015),inhibits tumor progress in nude mice KBV xenograft tumors model .
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- HY-113354S1
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Isotope-Labeled Compounds
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Neurological Disease
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Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-114169
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WRG-28
2 Publications Verification
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Discoidin Domain Receptor
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Inflammation/Immunology
Cancer
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WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
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- HY-155193
-
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Interleukin Related
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Inflammation/Immunology
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XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
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- HY-162312
-
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Deubiquitinase
Apoptosis
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Cancer
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LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
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- HY-P991528
-
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NF-κB
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Inflammation/Immunology
Cancer
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PE0116 is a fully human CD137 agonistic monoclonal antibody generated from immunized harbor H2L2 human transgenic mice. PE0116 is a ligand block. PE0116 activates NF-κB signaling which significantly promotes T-cell proliferation and increases cytokine secretion in vitro. PE0116 exhibits robust antitumor activity in MC38 tumor model .
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- HY-177406
-
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TNF Receptor
Apoptosis
NO Synthase
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Inflammation/Immunology
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VR11 aptamer is a DNA-based TNF-α inhibitor with a KD of 7.0 nM. VR11 aptamer prevents TNFα-induced apoptosis and NO production. VR11 aptamer has non-immunogenicity and does not raise immune responses when injected intraperitoneally into C57BL/6 mice model. VR11 aptamer can be used for inflammatory diseases research .
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- HY-125639
-
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(rac)-AR-13324 M1 metabolite
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PKC
ROCK
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Cardiovascular Disease
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(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .
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- HY-182579
-
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p38 MAPK
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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CBS-3408 is an orally active p38α MAPK inhibitor. CBS-3408 inhibits the release of TNFα and IL-1β. CBS-3408 reduces the disease severity of arthritis in mice. CBS-3408 inhibits TNFα release in a rat endotoxemia model. CBS-3408 can be used in studies related to endotoxemia and arthritis .
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- HY-170444
-
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Histamine Receptor
mAChR
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Neurological Disease
|
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ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models .
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- HY-108041
-
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BCI 838
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mGluR
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Neurological Disease
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MGS 0210 (BCI 838) is an orally active metabolite of glutamate receptor 2/3 (mGluR2/3) agonists. MGS 0210 improves amnesia and reduces anxiety in APP mice. MGS 0210 improves PTSD-related behaviors in a mouse model of post-traumatic stress disorder (PTSD). MGS 0210 can be used in research on neurological disorders such as Alzheimer's disease and major depressive disorder .
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- HY-157082
-
|
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Enterovirus
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Infection
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ZHSI-1 is an EV71 (Enterovirus 71) inhibitor that inhibits EV71/CVA16 replication and virus-induced pyroptosis associated with viral pathogenesis. ZHSI-1 effectively prevents EV71 infection in neonatal and young mice in animal models. ZHSI-1 can be used to study viral infections such as hand, foot and mouth disease (HFMD) .
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- HY-125327
-
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SGLT
|
Metabolic Disease
|
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YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.
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- HY-12443
-
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Casein Kinase
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Neurological Disease
|
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PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
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- HY-179701
-
|
|
NF-κB
TNF Receptor
Interleukin Related
CXCR
|
Inflammation/Immunology
|
|
NIK-IN-3 is a potent and orally active NF-κB-inducing kinase (NIK) inhibitor with an IC50 of 5.2 nM. NIK-IN-3 suppresses non-canonical NF-κB pathway activation and inhibits the secretion of pro-inflammatory cytokines, such as TNF-α, IL-6, IL-1β and chemokine CXCL12. NIK-IN-3 shows significant anti-inflammatory effects in LPS (HY-D1056)-induced sepsis mice model and DSS (HY-116282)-induced colitis model. NIK-IN-3 can be used for the research of inflammation, such as colitis .
|
-
- HY-125172
-
|
Polyglutamine Aggregation inhibitor III
|
Huntingtin
|
Others
|
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s=25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2 transgenic mouse model of Huntington's disease.
|
-
- HY-178147
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 52 is an orally active formation of synthetic hemozoin (β-hematin) inhibitor with an IC50 of 6.6 μM. Antimalarial agent 52 exhibits in vitro antiplasmodial activity against P. falciparum Pf3D7, PfDd2 strains and P. knowlesi with IC50s of 6.1, 6.4 and 3.3 nM. Antimalarial agent 52 remain highly effective against multidrug-resistant strains and demonstrates curative activity in the P. berghei mouse model .
|
-
- HY-125833
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
Apoptosis
|
Cancer
|
|
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis .
|
-
- HY-157457
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Z21090 (ZL40) is a potent inhibitor of PDE4 with the IC50 value of 37.4 nM and oral bioavailability. Z21090 plays an important role in alcohol-related diseases research .
|
-
- HY-125833R
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
Apoptosis
Reference Standards
|
Cancer
|
|
Alpha-Naphthoflavone (Standard) is the analytical standard of Alpha-Naphthoflavone. This product is intended for research and analytical applications. Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis .
|
-
- HY-174129
-
|
|
Btk
Apoptosis
|
Cancer
|
|
TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
|
-
- HY-N6605
-
|
Trifolin
|
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Kaempferol 3-O-β-D-galactopyranoside (Trifolin) is an orally active flavonoid derivative that can be found in the aerial parts of Consolida oliverana. Kaempferol 3-O-β-D-galactopyranoside exhibits antitumor and cardioprotective effects .
|
-
- HY-149984
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model .
|
-
- HY-178098
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-21 is a potent and orally active pan-TEAD inhibitor with an IC50 of 3 nM. TEAD-IN-21 effectively inhibited the proliferation of Huh-7 cells. TEAD-IN-21 selectively downregulates TEAD-dependent downstream genes. TEAD-IN-21 achieves tumor regression in a liver cancer-derived tumor xenograft mice model. TEAD-IN-21 can be used in the research of hepatocellular carcinoma (HCC) .
|
-
- HY-174819
-
|
|
HBV
|
Infection
|
|
VNRX-9945 is a potent, broadly and orally active HBV CAM (capsid assembly modulator) with an EC50 of 2.6 nM. VNRX-9945 exhibits excellent and broad antiviral activity against multiple HBV genotypes in vitro, along with favorable pharmacokinetic profiles across multiple species. VNRX-9945 demonstrates robust antiviral efficacy in the adeno-associated virus mice models of HBV (AAV-HBV) infection .
|
-
- HY-113365
-
|
4-Cholesten-3-one
|
Endogenous Metabolite
|
Infection
Metabolic Disease
|
|
Cholestenone (4-cholesten-3-one) is an orally available antimicrobial agent that is metabolized primarily in the liver as an intermediate oxidation product of cholesterol. Cholestenone inhibits human dermal fibroblast migration and fights Helicobacter pylori infection in vitro and in mouse models by inhibiting cholesterol-α-D-glucopyranoside (CGL). Cholestenone also alleviates metabolic disorders caused by obesity in db/db mice .
|
-
- HY-158315
-
|
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
|
|
NZ-97 is an inhibitor for dipeptidyl peptidase 4 (DPP4) with an IC50 of 18 nM. NZ-97 exhibits a low initial plasma exposure with Cmax of 0.13 µM, which is eliminated in 8 h. NZ-97 ameliorates damage in the Lipopolysaccharides (HY-D1056)-induced lung injury and Bleomycin (HY-108345)-induced lung fibrosis in mice model .
|
-
- HY-134923
-
|
|
Autophagy
|
Neurological Disease
|
|
CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in?lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's?disease research .
|
-
- HY-108790
-
|
Peginterferon β-1a
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Peginterferon beta-1a (Peginterferon β-1a) is the first pegylated interferon beta-1a molecule. Peginterferon beta-1a induces cancer cells apoptosis and shows anti-tumor activities in nude mice models. Peginterferon beta-1a can be used for the research of cancer and multiple sclerosis (RMS) .
|
-
- HY-116636
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
KRCA-0377 is an orally active ALK inhibitor with an IC50 of 0.001 μM. KRCA-0377 also inhibits mutant ALK enzyme with IC50 values ≤0.01 μM. KRCA-0377 shows cytotoxicity against cancer cells and inhibits tumor growth in xenograft mice models. KRCA-0377 can be used for the research of ALK-positive non-small-cell lung cancer .
|
-
- HY-164546
-
|
|
STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
|
-
- HY-126124
-
|
|
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
|
|
AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research .
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-175664
-
|
|
RPE65
|
Metabolic Disease
|
|
EYE-003 is an orally active RPE65 inhibitor with an IC50 of 102 nM. EYE-003 regulates the visual cycle in mice by reducing 11-cis-retinal (11cRAL) (HY-116711) synthesis and increasing all-trans-retinyl esters (atREs). EYE-003 suppresses scotopic ERG b-wave amplitude and exerts protective effects against retinal degeneration in Abca4 ⁻/⁻ Rdh8 ⁻/⁻ mice (a STGD1 model) by reducing retinal autofluorescent puncta and preserving outer nuclear layer (ONL) thickness in a dose-dependent manner. EYE-003 can be used for the study of visual cycle-associated retinopathies, such as Stargardt disease type 1 (STGD1) .
|
-
- HY-P990107
-
|
|
TGF-β Receptor
|
Cancer
|
|
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
|
-
- HY-177435
-
|
|
FAP
|
Inflammation/Immunology
|
|
FAPI-800CW is a near-infrared (NIR) fluorescent-labeled fibroblast activation protein (FAP) inhibitor. FAPI-800CW shows specific uptake in inflamed paws in collagen-induced arthritis (CIA) model mice. FAPI-800CW can be used for in vivo molecular imaging of FAP expression in inflammatory diseases such as rheumatoid arthritis (RA) to monitor joint inflammation and disease activity .
|
-
- HY-174847
-
|
|
p97
|
Cancer
|
|
VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC50 of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-15344
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
Metabolic Disease
|
|
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
|
-
- HY-N0088R
-
|
Acetovanillone (Standard)
|
Reference Standards
NADPH Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Apocynin (Standard) is the analytical standard of Apocynin. This product is intended for research and analytical applications. Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
|
-
- HY-P99583
-
|
MEDI4893
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
|
-
- HY-180582
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
QND8 is a selective and potent α7 nicotinic acetylcholine receptor (nAChR) agonist. QND8 can alleviate thermal hyperalgesia and mechanical hyperalgesia in carrageenan-induced inflammatory pain mouse model. QND8 can reduce the swelling of the mice feet, inhibit the release of pro-inflammatory factors at the inflammatory site, and prevent the infiltration of white blood cells. QND8 can be used for the research of inflammation and neurological disease, such as arthritis .
|
-
- HY-P10109
-
|
|
Glucose-6-Phosphate Isomerase (GPI)
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
-
- HY-152142
-
DN-1289
1 Publications Verification
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
|
-
- HY-15698A
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-121495
-
|
|
Parasite
|
Infection
|
|
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
|
-
- HY-168035
-
|
|
Histone Methyltransferase
|
Cancer
|
|
W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
|
-
- HY-P10109A
-
|
hG6PI (325-339) hydrochloride
|
Glucose-6-Phosphate Isomerase (GPI)
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) hydrochloride is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) hydrochloride primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) hydrochloride induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
-
- HY-15698
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-174308
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr .
|
-
- HY-103327R
-
|
|
Reference Standards
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 (Standard) is the analytical standard of MJ15 (HY-103327). This product is intended for research and analytical applications. MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-108841
-
Raleukin
Maximum Cited Publications
52 Publications Verification
Kineret; Anakinra
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Raleukin (AMG-719) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin significantly reduces neutrophil accumulation in blood vessels and brain infarct volume as well as improves motor coordination performance in ischemic stroke mice model. Anakinra can be used to study chronic inflammatory disorders like rheumatoid arthritis and cardiovascular recurrence post-myocardial infarction .
|
-
- HY-162640
-
|
|
ROR
|
Cancer
|
|
LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-146401
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice .
|
-
- HY-P990264
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4 +, CD8 + T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models .
|
-
- HY-173515
-
|
|
FAK
|
Cancer
|
|
FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 % .
|
-
- HY-14162
-
|
|
FLAP
|
Inflammation/Immunology
|
AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB4 and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma .
|
-
- HY-126477R
-
|
|
Reference Standards
Endogenous Metabolite
|
Cancer
|
|
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
|
-
- HY-165369
-
|
|
Aurora Kinase
|
Cancer
|
|
IBPR002 is an inhibitor of Aurora kinase A and Aurora kinase B, with IC50 values of 41 nM and 17 nM, respectively. IBPR002 disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and promotes the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to microtubules derived from the mother centrosome. IBPR002 reduces tumorigenesis levels in a colorectal cancer xenograft model using athymic nude mice. IBPR002 is applicable for research related to colorectal cancer .
|
-
- HY-155525
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-NASH agent 1 (compound 3d),a derivative of Elafibranor (HY-16737),is a potent agonist of PPAR-α/δ,targeting to nonalcoholic steatohepatitis (NASH). Anti-NASH agent 1 (3-10 mg/kg; 4 weeks) improves hyperlipidemia,liver fat degeneration and liver inflammation in Methionine-choline deficiency (MCD) induced NASH mice model. Anti-NASH agent 1 shows low liver toxicity and potent liver protection effect .
|
-
- HY-N6967R
-
|
(-)-α-Bisabolol (Standard)
|
Reference Standards
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-175465
-
|
|
Interleukin Related
STAT
|
Cancer
|
|
SMI-10B13 is an Oncostatin M (OSM) inhibitor with a KD of 6.6 μM. SMI-10B13 inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines (IC50 = 136 and 164 nM, respectively). SMI-10B13 shows anti-tumor effect in human breast cancer mice models .
|
-
- HY-158316
-
|
|
Fc Receptor (FcR)
|
Others
|
|
BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumin, low endotoxin (HY-W250978A)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
|
-
- HY-169120
-
|
|
Telomerase
|
Cancer
|
|
FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research .
|
-
- HY-18956A
-
|
(E/Z)-Sephin1 hydrochloride; (E/Z)-IFB-088 hydrochloride
|
Phosphatase
|
Neurological Disease
|
|
(E/Z)-Icerguastat hydrochloride ((E/Z)-Sephin1 hydrochloride) is a selective inhibitor with activity that prolongs the phosphorylation effects of eIF2α. (E/Z)-Icerguastat hydrochloride protects cells from defects in proteostasis. (E/Z)-Icerguastat hydrochloride was shown to significantly extend the survival of infected prion mice in a mouse model. (E/Z)-Icerguastat hydrochloride effectively reduces PrPSc expression and prion sequence activity in various neuronal cell lines persistently infected with different prion strains .
|
-
- HY-176063
-
|
|
TRP Channel
Opioid Receptor
|
Neurological Disease
|
|
TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-170232
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-29 (Compound 22) is a RIPK1 inhibitor, with an IC50 of 6.9 nM. RIPK1-IN-29 exerts anti-necroptotic (Apoptosis) activity by inhibiting RIPK1. In a TNF-α-induced in vivo inflammation model, at a dose of 10 mg/kg, RIPK1-IN-29 can protect mice from hypothermia and death. RIPK1-IN-29 can be applied to the research field of inflammatory diseases .
|
-
- HY-124727
-
|
|
JAK
Apoptosis
|
Cancer
|
|
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
|
-
- HY-149838
-
|
|
NF-κB
|
Cancer
|
|
NF-κB-IN-9 is a nuclear factor kappa B (NF-κB) targeting sonosensitizer (λex/λem=489/628 nm). NF-κB-IN-9 exhibits strong inhibition on NF-κB signaling due to its two resveratrol units in one molecule. NF-κB-IN-9 has anti-tumor activity and shows remarkable sonocytotoxicity against cancer cells. NF-κB-IN-9 has biosafety in eenograft mice model.
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-
- HY-162710
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC50 of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models .
|
-
- HY-118282
-
|
|
PGE synthase
|
Endocrinology
|
|
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice .
|
-
- HY-P5875
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
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-
- HY-P11603
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
SK56 is a GSDMD-NT pore inhibitor. SK56 inhibits pyroptosis (Pyroptosis) and the release of pyroptosis-related cytokines in macrophages and human peripheral blood leukocytes. SK56 prevents extensive cell death in human alveolar organoids in an organoid-macrophage co-culture model. SK56 prevents death from infectious shock induced by LPS (HY-D1056) or cecal ligation and puncture in mice. SK56 can be used in studies related to sepsis .
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-
- HY-15698B
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-P11208
-
|
|
GABA Receptor
|
Inflammation/Immunology
|
|
mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .
|
-
- HY-167706
-
|
|
GPR35
|
Inflammation/Immunology
|
|
Diethyl-Lodoxamide is a highly potent GPR35 agonist with potential to inhibit inflammatory bowel disease. Diethyl-Lodoxamide activates GPR35 in humans, mice and rats, showing similar EC50 values. Diethyl-Lodoxamide can alleviate the clinical symptoms of DSS-induced inflammatory bowel disease in mouse models, and the effect is better than the traditional drug 5-ASA. The pharmaceutical properties of Diethyl-Lodoxamide have been optimized to better meet the requirements of drug design .
|
-
- HY-153808
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
|
-
- HY-17555
-
|
Centrophenoxine hydrochloride
|
nAChR
iGluR
|
Neurological Disease
|
|
Meclofenoxate (Centrophenoxine) hydrochloride is an ester synthesized from DMAE and pCPA, capable of crossing the blood-brain barrier, and can stimulate memory and enhance cognition .
|
-
- HY-156083
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors .
|
-
- HY-103450R
-
|
|
Reference Standards
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
G36 (Standard) is the analytical standard of G36 (HY-103450). This product is intended for research and analytical applications. G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
- HY-103450
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
|
-
- HY-175547
-
|
|
PROTACs
MAP4K
ERK
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader (DC50 = 5.0 nM; Dmax ≥ 99%). PROTAC HPK1 Degrader-5 significantly inhibits SLP76 phosphorylation and enhanced ERK pathway activation through degrading HPK1, thereby stimulating IL-2 and IFN-γ release. PROTAC HPK1 Degrader-5 exhibits the ability to overcome the immunosuppressive effects imposed by PGE2, NECA or TGF-β. PROTAC HPK1 Degrader-5 alone efficaciously inhibits tumor growth in an MC38 syngeneic mouse model. PROTAC HPK1 Degrader-5 can be used for the study of tumor (such as colorectal cancer) immunotherapy (Pink: Target protein ligand (HY-175549); Blue: E3 ligand (HY-W023573); Black: Linker; E3 ligand + Linker (HY-175551)) .
|
-
- HY-A0021
-
|
|
5-HT Receptor
Flavivirus
|
Infection
Cardiovascular Disease
Neurological Disease
|
|
Palonosetron hydrochloride is a 5-HT3 antagonist primarily used to prevent acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition, Palonosetron hydrochloride exhibits moderate anti-flavivirus activity and potent anti-Zika virus activity in mammalian cells. Palonosetron hydrochloride also possesses antidepressant activity .
|
-
- HY-P991637
-
|
|
Ser/Thr Protease
|
Metabolic Disease
|
|
REGN7999 is a monoclonal antibody that inhibits TMPRSS6. REGN7999 inhibits TMPRSS6 activity, preventing Hemojuvelin (HJV) lysis, thereby enhancing BMP6-HJV signaling and increasing serum hepcidin. REGN7999 ameliorates iron overload and impaired erythropoiesis in a β-thalassemia mouse model by inhibiting TMPRSS6 activity. REGN7999 is indicated for research in β-thalassemia .
|
-
- HY-N6973
-
Boldine
1 Publications Verification
|
RANKL/RANK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research .
|
-
- HY-W012980R
-
|
|
Reference Standards
Endogenous Metabolite
AMPK
PKA
|
Metabolic Disease
|
|
Isovaleric acid (Standard) is the analytical standard of Isovaleric acid. This product is intended for research and analytical applications. Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
|
-
- HY-W012980
-
|
|
Environmental Pollutants
Endogenous Metabolite
PKA
AMPK
|
Metabolic Disease
|
|
Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
|
-
- HY-P99022
-
|
R-04909832; RG-1450
|
Amyloid-β
|
Neurological Disease
|
|
Gantenerumab is a fully humanized anti-Aβ IgG1 monoclonal antibody. Gantenerumab can specifically bind to Aβ fibrils and plaques and can be used in Alzheimer's disease research .
|
-
- HY-N0469A
-
|
|
Endogenous Metabolite
Virus Protease
|
Inflammation/Immunology
Cancer
|
|
L-lysine sulfite is an essential amino acid for humans , offers numerous benefits and can be used in herpes research. Additionally, L-lysine sulfite enhances calcium absorption, reduces diabetes-related complications, improves gut health, and alleviates pancreatitis inflammation .
|
-
- HY-175248
-
|
|
PSMA
|
Cancer
|
|
PSMA-DIM is a dimeric PSMA ligand with a Kd of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [ 68Ga]Ga to form [ 68Ga]Ga-PSMA-DIM. [ 68Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [ 68Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa) .
|
-
- HY-177497
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2 MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer .
|
-
- HY-N1420
-
|
L-Rhamnose
|
Environmental Pollutants
Endogenous Metabolite
PKA
MMP
Interleukin Related
|
Infection
Metabolic Disease
Cancer
|
|
Rhamnose (L-Rhamnose ) is an orally active deoxysugar. Rhamnose can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
- HY-183284
-
|
|
FAK
ERK
Apoptosis
|
Neurological Disease
Cancer
|
|
GZD-552 is a potent orally active FAK inhibitor with a human FAK IC50 of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G2/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme .
|
-
- HY-172455
-
|
|
Potassium Channel
|
Neurological Disease
|
|
TREK inhibitor-3 (Cpd8l) is a selective and BBB-permeable TREK-1 inhibitor with an IC50 of 0.81 μM. TREK inhibitor-3 has neuroprotective effects, which can significantly reduce the death of cortical neurons induced by oxygen-glucose deprivation/reoxygenation (OGD/R) and improve brain injury in mice models of middle cerebral artery occlusion/reperfusion (MCAO/R). TREK inhibitor-3 can be used in the research of ischemic stroke .
|
-
- HY-173160
-
|
|
HDAC
|
Cancer
|
|
HDAC1-IN-10 (Compound 2b) is a potent, selective and orally active HDAC1/2 inhibitor with IC50 values of 6 and 190 nM. HDAC1-IN-10 shows IC50 > 50 μM for HDAC3-8. HDAC1-IN-10 can inhibit tumor growth in HCT-116 colon xenograft nude mice model. HDAC1-IN-10 can be used for research of colon cancer .
|
-
- HY-151155
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
|
-
- HY-150562
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-175342
-
|
LOXO-338
|
Bcl-2 Family
|
Cancer
|
|
FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL .
|
-
- HY-B1350A
-
|
Sodium fusidate; SQ-16360
|
Bacterial
Antibiotic
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Fusidic acid sodium salt is an orally available antibacterial agent that inhibits bacterial protein synthesis by preventing the release of translation elongation factor G (EF-G) from ribosomes. Fusidic acid sodium salt inhibits the inhibitory and activating effects of interleukins IL-1 and IL-6 on glucose-induced insulin production and exhibits antidiabetic effects in a rat model. Fusidic acid sodium salt improves the symptoms of colitis in rats and inhibits the growth of Toxoplasma gondii and Listeria monocytogenes EGD in vitro, but not in mice .
|
-
- HY-172826
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 26 is a potent anti-MRSA agent with MIC <0.015 μg/mL. Anti-MRSA agent 26 has superior activity against a broad range of Gram-positive pathogens and shows no cytotoxicity in three mammalian cell lines (Caco-2, DU-145 and MDCKII MDR1 cells) at 10 μM. Anti-MRSA agent 26 has a robust TAP pharmacophore and an excellent antibacterial activity in Staphylococcus aureus skin infection mice model .
|
-
- HY-N1420A
-
|
L-Rhamnose monohydrate
|
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
Infection
Metabolic Disease
Cancer
|
|
Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
- HY-149648
-
|
|
RSV
DNA/RNA Synthesis
|
Infection
|
|
JNJ-8003 is a potent and orally active non-nucleoside RSV polymerase inhibitor with an IC50 of 0.29 nM. JNJ-8003 targets the L protein polymerase complex of RSV (IC50 = 0.67 nM), and blocks the transcription and replication of the viral genome by inhibiting the activity of RNA-dependent RNA polymerase (RdRp). JNJ-8003 displays subnanomolar activity in vitro as well as prominent efficacy in mice and a neonatal lamb models. JNJ-8003 can be used for the study of respiratory syncytial virus (RSV) .
|
-
- HY-P11262
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GUB021794 is a potent and highly selective glucagon-like peptide-1 receptor (GLP-1R) agonist developed using the streaMLine platform with an EC50 value of 18 pM. GUB021794 has a very weak activity against SCTR, with an EC50 value of 190 nM. GUB021794 can significantly reduce the body weight, food intake, and total fat mass of mice in a diet-induced obesity (DIO) model. GUB021794 can be used for research on obesity/diabetes .
|
-
- HY-162645
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
|
-
- HY-101117
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
|
-
- HY-170237
-
|
|
Salt-inducible Kinase (SIK)
|
Cancer
|
|
SIK2/3-IN-1 (Compound 7S) is a selectively inhibitory agent of SIK2/3 with oral activity. SIK2/3-IN-1 can significantly inhibit tumor growth (without any body weight loss) in the MV4-11 AML mice CDX model. SIK2/3-IN-1 can be used in the research of MEF2C-dependent acute myeloid leukemia .
|
-
- HY-162919
-
|
|
CDK
Apoptosis
c-Myc
|
Cancer
|
|
YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia .
|
-
- HY-177933
-
|
|
CCR
|
Neurological Disease
Inflammation/Immunology
|
|
mNOX-E36 is a murine-specific analogue of NOX-E36 (HY-148100), an anti-CCL-2 L-RNA aptamer that binds and neutralises the mouse chemokine CCL-2. mNOX-E36 reduces scarring in an experimental murine model of glaucoma filtration surgery (GFS). mNOX-E36 ameliorates lupus nephritis in mice. mNOX-E36 can be used for GFS and lupus nephritis research .
|
-
- HY-150596
-
|
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-P99124
-
|
|
CD3
|
Inflammation/Immunology
|
|
Anti-Mouse CD3 Antibody (17A2) is an anti-mouse CD3 IgG2b antibody inhibitor derived from the host Rat. Anti-Mouse CD3 Antibody (17A2) enhances T-cell proliferation and activation and stimulate IFN-γ or IL-17 production in splenic T cells. Anti-Mouse CD3 Antibody (17A2) significantly suppresses mortality in Graft-versus-host disease (GVHD) mice models .
|
-
- HY-111837
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
Bcl-2 Family
|
Cancer
|
|
BI1071 is an orally active Nur77-Bcl-2 apoptotic pathway modulator. BI1071 can bind to Nur77-LBD protein with a Kd of 0.17 μM. BI1071 can activate Nur77 signaling and induce apoptosis by translocating to mitochondria where it interacts with Bcl-2. BI1071 can inhibit tumor growth in SW620 xenograft mice model. BI1071 can be used for research of colon cancer .
|
-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
|
-
- HY-100591
-
|
|
Sirtuin
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
|
-
- HY-P991570
-
|
AD5-10; oba-01 Antibody
|
TNF Receptor
Apoptosis
Caspase
Atg8/LC3
Akt
Beclin1
JNK
|
Cancer
|
|
Zaptuzumab (AD5-10) is a DR5-specific humanized monoclonal antibody that selectively binds to DR5 with high affinity. Zaptuzumab specifically induces cancer cell death by both caspase-apoptosis and autophagic cell death (ACD). Zaptuzumab activates both ADCC and CDC. Zaptuzumab induces ROS generation and GSH level reduction. Zaptuzumab shows a significant suppression of the tumor growth and good safety in various xenografts mice tumor models .
|
-
- HY-181146
-
|
TBD09
|
Bacterial
|
Infection
|
|
MK-7762 is an orally active xazolidinone compound with antitubercular activity. MK-7762 inhibits MAO-B and mammalian mitochondrial protein synthesis. MK-7762 reduces lung bacterial burden in BALB/c mouse models of acute and chronic tuberculosis infection, penetrates caseous necrotic lung lesions in C3HeB/FeJ mice, and maintains concentrations above unbound MIC in lesion compartments. MK-7762 can be used for the research of tuberculosis .
|
-
- HY-161834
-
|
|
Pyroptosis
Aquaporin
NOD-like Receptor (NLR)
p38 MAPK
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
RG100204 is a selective, orally available inhibitor of the aquaporin AQP9. RG100204 directly inhibits AQP9 channel function, preventing the transmembrane transport of water, glycerol, and H 2O 2. RG100204 reduces the activation of the NLRP3 inflammasome and p38 MAPK signaling pathways, thereby alleviating inflammation and pyroptosis. RG100204 reduces multi-organ dysfunction in a mouse sepsis model and shows glucose-regulating effects in diabetic db/db mice .
|
-
- HY-P992352
-
|
|
|
|
|
ES005 is an anti-tumor compound and LAG3 inhibitor. ES005 blocks the interactions of LAG3 with MHC-II, LSECtin and FGL1, thereby effectively reversing the LAG3-mediated inhibition of T cell activation and NFAT reporter gene expression. ES005 exhibits significant tumor growth inhibitory effects in syngeneic mouse breast tumor models using humanized LAG3 knock-in mice. ES005 can be used for breast tumor-related research .
|
-
- HY-107202
-
-
- HY-107202GL
-
|
Poly(I:C) (GMP Like)
|
Toll-like Receptor (TLR)
PKD
HSP
Bcl-2 Family
Interleukin Related
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
|
-
- HY-107202A
-
-
- HY-P10868
-
|
RLS-0071
|
Reactive Oxygen Species (ROS)
|
Infection
Inflammation/Immunology
|
|
Pegtarazimod (RLS-0071) is a dual-target anti-inflammatory peptide that exerts its effects by simultaneously regulating the complement system and neutrophil-associated inflammatory pathways. Pegtarazimod reduces ROS production both in vitro and in vivo, and decreases the level of neutrophil elastase, a marker of neutrophil extracellular traps (NETs), in vivo, thereby alleviating inflammatory responses. Pegtarazimod significantly improves the survival rate of mice in multiple in vivo models of acute graft-versus-host disease (aGVHD). Pegtarazimod inhibits the activation of the C1 complex, reduces the herpes zoster-like spread of herpes simplex virus type 1 skin infection, and improves the survival rate of infected mice . Pegtarazimod can be used in research related to acute graft-versus-host disease, acute pulmonary diseases, and skin herpes simplex virus type 1 infection .
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-
- HY-163121
-
|
|
Glycosyltransferase
TGF-β Receptor
FAK
Galectin
Collagen
|
Endocrinology
Cancer
|
|
PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease .
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-
- HY-175294
-
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|
PD-1/PD-L1
NAMPT
|
Cancer
|
|
PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma .
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-
- HY-170321
-
|
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Apoptosis
|
Cancer
|
|
Apoptosis inducer 31 (compound 19) induces caspase-dependent apoptosis. Apoptosis inducer 31 plays an important role in cancer research .
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-
- HY-19480
-
|
BCX4208
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Ulodesine is a purine nucleoside phosphorylase (PNP) inhibitor. Ulodesine inhibits PNP with IC50 value of 2.293 nM/L. Ulodesine can be used for the research of hyporucicemia .
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-
- HY-173558
-
|
|
PD-1/PD-L1
HDAC
Apoptosis
|
Cancer
|
|
PD-L1/HDAC3-IN-1 (PH3) is a dual PD-L1/HDAC3 Inhibitor with IC50 values of 89.4 nM and 107 nM for PD-1/PD-L1 and HDAC3, respectively. PD-L1/HDAC3-IN-1 induces cell apoptosis and arrests cell cycle at G0/G1 phase. PD-L1/HDAC3-IN-1 shows anticancer activity both in vivo and in vitro .
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-
- HY-123972
-
|
KL-2
|
DNA/RNA Synthesis
|
Cancer
|
|
SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .
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-
- HY-175215
-
|
|
Parasite
|
Infection
|
|
PfPK6-IN-1 is a potent and selective PfPK6 inhibitor with an IC50 of 0.3 μM. PfPK6-IN-1 inhibits hemozoin formation, a Plasmodium-specific pathway with IC50 of 13 μM against β-hematin (βH). PfPK6-IN-1 exhibits rapid and broad-spectrum anti-malarial properties, being effective against both chloroquine-sensitive and resistant strains.PfPK6-IN-1 can be used for the study of antimalarial .
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- HY-N14001
-
|
|
TNF Receptor
Interleukin Related
Arginase
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Naamidine J is an imidazole-type alkaloids discovered in a sponge. Naamidine J inhibits inflammation by binding to the protein CSE1L (KD = 5.41 μM). Namidine J significantly inhibits the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and upregulates anti-inflammatory factors such as CD206 and Arg-1. Namidine J inhibits PD-L1 and shows antitumor activity. Namidine J significantly reduces pulmonary tissue edema, inflammatory cell infiltration and cytokine storm in mice. Namidine J can be used for the research on the immune microenvironment of acute lung injury and tumors .
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-
- HY-174989
-
|
|
ATM/ATR
Apoptosis
|
Cancer
|
|
ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer .
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-
- HY-N0217
-
-
- HY-175232
-
|
|
Nuclear Factor of activated T Cells (NFAT)
Endogenous Metabolite
|
Endocrinology
|
|
GL64 is a selective agonist of ADGRD1 (EC50 = 3.98 μM). GL64 has low selectivity for ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4 isoforms. GL64 activates ADGRD1 by mimicking the satchel sequence. GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway. GL64 effectively inhibits osteoclastogenesis and prevents bone loss both in vitro and in vivo. GL64 is useful in the study of osteoclast-related diseases .
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-
- HY-175537
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. ATX-IN-3 certainly reduces collagen deposition and ameliorates lung fibrosis in the pulmonary fibrosis mouse model. ATX-IN-3 has good metabolic stability and drug-like properties. ATX-IN-3 can used for the study of idiopathic pulmonary fibrosis (IFP) .
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-
- HY-117006
-
E1231
1 Publications Verification
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
|
Sirtuin
|
Cardiovascular Disease
|
|
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
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- HY-161833
-
|
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Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
HSP90-IN-31 (compound Be01) causes reduction of CD80 and CD86 expression on dendritic cells (DCs). HSP90-IN-31 decreases the production of pro-inflammatory cytokines (IL-6, TNF-α, and IL-1β) in BMDC and peritoneal macrophages stimulated by LPS (HY-D1056). Under the delayed-type hypersensitivity (DTH) mice model, HSP90-IN-31 reduces ear swelling and pro-inflammatory cytokines in the spleen .
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-
- HY-149862
-
|
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PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
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-
- HY-164102
-
|
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TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
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-
- HY-153369
-
|
BAY 1165747
|
Guanylate Cyclase
|
Cardiovascular Disease
Neurological Disease
|
|
BAY-747 (BAY 1165747) is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model .
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-
- HY-143880
-
|
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Mas-related G-protein-coupled Receptor (MRGPR)
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Neurological Disease
|
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
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-
- HY-N12087
-
|
|
NF-κB
NO Synthase
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
8-Deoxylactucin is an orally active sesquiterpene lactone. 8-Deoxylactucin inhibits LPS (HY-D1056)-induced NO production in RAW264.7 macrophages with an IC50 value of 4.35 μM. 8-Deoxylactucin exerts anti-inflammatory effects by blocking the NF-κB pathway. 8-Deoxylactucin demonstrates hepatoprotective efficacy in LPS/D-galactosamine-induced acute hepatitis model of mice. 8-Deoxylactucin can be used for the study of inflammatory diseases and inflammatory liver injuries .
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-
- HY-118424
-
|
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iGluR
|
Neurological Disease
Metabolic Disease
|
|
JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures .
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-
- HY-120015
-
|
|
MMP
|
Cancer
|
|
BE-16627B is a metalloproteinase inhibitor. BE-16627B can be isolated from microbial cultures. BE-16627B can inhibit metalloproteinases in enzyme assays. BE-16627B reduces the number and size of HT1080 cell nodules on lung surface in mouse models. BE-16627B inhibits growth of HT1080 cells in mice. BE-16627B can be studied in anti-cancer research .
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-
- HY-159925
-
|
|
Cyclic GMP-AMP Synthase
|
Infection
Inflammation/Immunology
|
|
QKY-613 is a prodrug that enhances immune surveillance by targeting nucleic acid modification pathways. QKY-613 promotes the selective incorporation of 6mdA (N6-methyldeoxyadenosine) into viral DNA, enhancing the phase separation potential of DNA, thereby increasing the activation of cGAS and strengthening host immune surveillance. In virus-infected mouse models, QKY-613 significantly reduced mortality in aged mice. QKY-613 holds promise for research on nucleic acid modification-based immune surveillance mechanisms .
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-
- HY-178153
-
|
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iGluR
|
Neurological Disease
|
|
BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .
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-
- HY-162033
-
|
|
Chloride Channel
|
Others
|
|
PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF .
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-
- HY-P1408
-
|
|
Integrin
VEGFR
|
Cancer
|
|
Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma .
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-
- HY-175277
-
|
|
Pim
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
PIM1-IN-8 is a PIM1/p65 pathway inhibitor. PIM1-IN-8 suppresses the expression of α-SMA and collagen I in activated fibroblasts and blocks TGF-β induced migration. PIM1-IN-8 alleviates pulmonary fibrosis in a Bleomycin (BLM) (HY-17565A)-induced pulmonary fibrosis mice model. PIM1-IN-8 can be used for the study of idiopathic pulmonary fibrosis (IPF) .
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-
- HY-145586A
-
|
ZSP1273 monohydrate
|
Influenza Virus
DNA/RNA Synthesis
|
Infection
|
|
Onradivir (ZSP1273) monohydrate is an orally active antiviral agent targeting influenza A virus RNA polymerase PB2 subunit with an IC50 of 0.562 nM. Onradivir monohydrate inhibits cap binding to influenza A virus RNA polymerase PB2 subunit, suppresses viral replication, reduces viral titres and RNA loads, and inhibits influenza A virus infection. Onradivir monohydrate maintains high survival rates in influenza A virus-infected mice, and reduces influenza A virus titers in a murine model. Onradivir monohydrate can be used for the research of influenza A virus infection .
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-
- HY-173129
-
|
|
NF-κB
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 97 (Compound 1l), an anti-inflammation agent, can also inhibit oxidative stress. Anti-inflammatory agent 97 can inhibit the colonic shortening and suppress inflammatory symptoms of the colonic tissue in the DSS (HY-116282C)-induced ulcerative colitis mice model. Anti-inflammatory agent 97 can regulate the inflammation-related TLR4/NF-κB signaling pathway and the oxidative stress-related Nrf2/HO-1 signaling pathway .
|
-
- HY-139659
-
|
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-111817A
-
|
|
Parasite
|
Infection
|
|
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.
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-
- HY-168773
-
|
|
EAAT
|
Neurological Disease
|
|
(R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. (R)-AS-1 (at doses of 60 and 90 mg/kg) increases spontaneous locomotor activity in mice. Additionally, it demonstrates anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electrical stimuli (32 or 44 mA), with ED50s of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. (R)-AS-1 can be used in neurological disease research .
|
-
- HY-145586
-
|
ZSP1273
|
Influenza Virus
DNA/RNA Synthesis
|
Infection
|
|
Onradivir (ZSP1273) is an orally active antiviral agent targeting influenza A virus RNA polymerase PB2 subunit with an IC50 of 0.562 nM. Onradivir inhibits cap binding to influenza A virus RNA polymerase PB2 subunit, suppresses viral replication, reduces viral titres and RNA loads, and inhibits influenza A virus infection. Onradivir maintains high survival rates in influenza A virus-infected mice, and reduces influenza A virus titers in a murine model. Onradivir can be used for the research of influenza A virus infection .
|
-
- HY-174802
-
|
|
Cyclic GMP-AMP Synthase
IKK
IFNAR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
|
-
- HY-122830
-
|
|
PROTACs
Btk
NF-κB
|
Cardiovascular Disease
Cancer
|
|
DD-03-171 is a PROTAC BTK degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC50 = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717)) .
|
-
- HY-181604
-
|
|
Malate Dehydrogenase (MDH)
|
Inflammation/Immunology
|
|
MDH2-IN-2 is an orally active MDH2 inhibitor with an IC50 of 5.9 μM. MDH2-IN-2 reduces the levels of senescence markers and senescence-associated secretory phenotype (SASP) factors in mammalian cell models. MDH2-IN-2 extends the lifespan and improves the healthspan of Caenorhabditis elegans. MDH2-IN-2 alleviates tissue senescence in aged mice, inhibits SASP factors, and restores liver and kidney functions. MDH2-IN-2 is applicable for senescence-related research .
|
-
- HY-P11208C
-
|
|
GABA Receptor
|
Inflammation/Immunology
|
|
mNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .
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-
- HY-172887
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC50: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models .
|
-
- HY-170377
-
|
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
|
ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model .
|
-
- HY-172135
-
|
|
p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-26 (Compound A5) is an orally active and highly selective PDE4 inhibitor. PDE4-IN-26 has anti-inflammatory activity and can inhibit the phosphorylation of p38 MAPK. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 can improve pulmonary inflammation, injury and fibrosis, promote sputum secretion and relieve cough in mice. PDE4-IN-26 can be used for the research of lung injury-related diseases .
|
-
- HY-113898
-
|
|
Angiotensin-converting Enzyme (ACE)
Toll-like Receptor (TLR)
Interleukin Related
|
Cardiovascular Disease
Neurological Disease
|
|
Ganoderic acid K is a triterpenoid compound. Ganoderic acid K can be isolated from Ganoderma lucidum. Ganoderic acid K inhibits ACE activity with an IC50 of 2.6×10 -5 M. Ganoderic acid K exhibits direct, high-affinity binding to recombinant MD2 protein, with a Kd value of 0.47 μM. It potently inhibits LPS-induced release of TNF-α and IL-6. It reduces cerebral infarction volume and ameliorates neurological dysfunction in mice with ischemic stroke in the tMCAO model. Ganoderic acid K can be used in studies related to hypertension and ischemic stroke .
|
-
- HY-180802
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
|
BCFTP is a potent, orally active and selective human Mas-related G protein-coupled receptor X1 (MrgprX1)-positive allosteric modulator. BCFTP selectively potentiates MrgprX1 signaling in HEK293 cells. BCFTP alleviates specific neuropathic pain-related behaviors in a humanized MrgprX1 mouse model of chronic constrictive injury (CCI) in a MrgprX1-dependent manner. BCFTP synergistically enhances psychoactive substances analgesia in CCI MrgprX1 mice. BCFTP can be used for neuropathic pain research .
|
-
- HY-173116
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
DOTA-XYIMSR-01 is a molecular probe targeting CAIX that can be labeled with 177Lu for the inhibition and localization of malignant gliomas. The uptake of [177Lu] Lu-XYIMSR-01 in U87MG tumors is 6.19 % of the injected dose per gram (% ID/g), and the tumor-to-muscle uptake ratio is 20.14. In the orthotopic glioma model, combined injection with Temozolomide (HY-17364) can significantly improve the survival rate of mice and inhibit tumor growth. DOTA-XYIMSR-01 shows promise for research in the field of anti-cancer therapy .
|
-
- HY-10109A
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
AS-605240 (potassium) is an orally active PI3Kγ inhibitor (IC50: 8 nM; Ki: 7.8 nM). AS-605240 (potassium) inhibits MCP-1- and CSF1-induced PKB phosphorylation (IC50 values are 0.181 and 0.550 µM, respectively). AS-605240 (potassium) reduces neutrophil recruitment in RANTES (CCL5)- and thioglycolate-induced peritonitis mouse models (EC50 values are 9.1 and 10 mg/kg, respectively). AS-605240 (potassium) ameliorates αCII-IA-induced arthritis in mice .
|
-
- HY-N1420AR
-
|
L-Rhamnose monohydrate (Standard)
|
Reference Standards
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
Infection
Metabolic Disease
Cancer
|
|
Rhamnose monohydrate (Standard) is the analytical standard of Rhamnose monohydrate (HY-N1420A). Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
- HY-155226
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
|
-
- HY-117707
-
|
|
Raf
|
Cancer
|
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
|
-
- HY-121554
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Kojic amine is an orally active γ-aminobutyric acid (GABA) analog. Kojic amine acts as a GABA mimic that inhibits sodium-independent [ 3H]GABA binding to rat brain cell membranes. Kojic amine reduces flexor spasms in chronic spinal rat and cat models. Kojic amine prevents tonic extensor convulsions in mice. Kojic amine produces a transient, dose-dependent analgesic effect in the mouse hot-plate test. Kojic amine can be used in research related to skeletal muscle spasm, epilepsy and analgesia [1][2]
|
-
- HY-148291
-
|
|
LPL Receptor
Phosphodiesterase (PDE)
|
Cancer
|
|
BrP-LPA sodium is a pan-opposite agent for lysophosphatidic acid (LPA). It has antagonistic activity against LPA1 (IC50 = 4520 nM), LPA2 (IC50 = 468 nM), LPA3, and LPA4. BrP-LPA sodium also has partial agonistic activity for LPA5, with its EC50 being 1282 nM. BrP-LPA sodium has ATX inhibitory activity. BrP-LPA sodium effectively inhibits the migration and invasion of breast cancer cells. BrP-LPA sodium achieves tumor regression and anti-angiogenesis in mice breast cancer xenograft model. BrP-LPA sodium can be used for the study of breast cancer .
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-
- HY-107513
-
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mGluR
|
Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
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-
- HY-122179
-
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TGF-β Receptor
|
Inflammation/Immunology
|
|
NUCC-555 is an activin antagonist. NUCC-555 interacts with Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107 in the Activin A binding pocket. NUCC-555 blocks Activin A-mediated hepatic stellate cells (HSCs) activation. NUCC-555 promotes liver regeneration and halts fibrosis progression in chronic liver disease models. NUCC-555 inhibits Activin A-mediated ovarian cell proliferation. NUCC-555 decreases FSH levels in ovariectomized mice .
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- HY-P990181
-
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Glutathione Peroxidase
STING
|
Inflammation/Immunology
|
|
Anti-Mouse myeloperoxidase/MPO Antibody (6G4) is an anti-mouse myeloperoxidase/MPO IgG2c monoclonal antibody. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) can activate the cGAS/STING pathway. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) induces acute and chronic kidney injury in mice. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) is often used in the construction of inflammation conditions models such as anti-neutrophil cytoplasmic antibody (ANCA)-associated vasculitides (AAV) .
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- HY-175746
-
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CX3CR1
|
Cardiovascular Disease
|
|
AZD0233 is an orally active CX3CR1 antagonist. AZD0233 modulates the CX3CR1/CX3CL1 signaling axis via immunomodulatory effects. AZD0233 has improved physicochemical properties, metabolic stability, low toxicity and CYP inhibition. AZD0233 improves cardiac function and reduces macrophages and fibrotic scar in mice model of dilated cardiomyopathy. AZD0233 can be used for cardiovascular diseases like dilated cardiomyopathy research .
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-
- HY-17484
-
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CP 65703
|
Drug Derivative
|
Inflammation/Immunology
|
|
Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases .
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- HY-160421
-
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Apoptosis
|
Inflammation/Immunology
Cancer
|
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TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206 + and CX3CR1 + immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells .
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- HY-114900
-
|
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Antibiotic
|
Infection
Others
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|
BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research .
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- HY-P991294
-
|
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ADC Antibody
|
Cancer
|
|
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .
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- HY-P990116
-
|
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Osteopontin
|
Inflammation/Immunology
|
|
Anti-Mouse osteopontin/SPP1 Antibody (103D6) is a mouse-derived anti-mouse osteopontin/SPP1 IgG2c κ type antibody inhibitor. Anti-Mouse osteopontin/SPP1 Antibody (103D6) increases cytotoxic T lymphocyte lytic activity and suppresses colon tumor growth. Anti-Mouse osteopontin/SPP1 Antibody (103D6) ameliorates liver injury in common bile duct ligation (CBDL)-induced primary sclerosing cholangitis mice models .
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-
- HY-162600
-
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CDK
|
Inflammation/Immunology
|
|
CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases .
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-
- HY-N0918R
-
|
Demethoxyyangonin (Standard); 5,6-Dehydrokavain (Standard)
|
Reference Standards
Monoamine Oxidase
JAK
STAT
NO Synthase
IKK
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
|
Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123 µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation .
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-
- HY-163612
-
|
|
ROR
Apoptosis
|
Cancer
|
|
XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
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-
- HY-175321
-
|
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PROTACs
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC50s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer (Pink: c-Met ligand (HY-W425461); Blue: E3 ligand (HY-14658); Black: Linker (HY-20797)) .
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-
- HY-163611
-
|
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ROR
|
Cancer
|
|
XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro .
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-
- HY-110120
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect .
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-
- HY-175750
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
MOMA-341 is a selective Werner RecQ like helicase (WRN) inhibitor. MOMA-341 binds to WRN at cysteine 727 through an allosteric and ATP-competitive binding mechanism. MOMA-341 has antitumor activity and can be used for advanced and metastatic solid tumors research .
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-
- HY-162606
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases .
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-
- HY-175254
-
|
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Bacterial
|
Infection
|
|
Antibiofilm agent-17 is a dual-action biofilm inhibitor against Pseudomonas aeruginosa (IC50 = 0.33 μM). Antibiofilm agent-17 inhibits biofilm growth by reducing quorum sensing-mediated virulence production and iron ion acquisition. Antibiofilm agent-17 exhibits synergistic antimicrobial effects in a mouse wound infection model. Antibiofilm agent-17 can be used in research on combating Pseudomonas aeruginosa infections .
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-
- HY-157839
-
|
|
PROTACs
α-synuclein
Tau Protein
|
Neurological Disease
|
|
PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with KDs of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)) .
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- HY-N0469
-
|
|
Endogenous Metabolite
Virus Protease
HSV
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
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-
- HY-146780
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model .
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-
- HY-17015
-
-
- HY-17015A
-
|
RWJ-270201; BCX-1812
|
IKK
JNK
STAT
p38 MAPK
ERK
|
Infection
Inflammation/Immunology
|
|
Peramivir is an novel cyclopentane neuraminidase inhibitor of influenza virus. Peramivir has antiviral activity and anti-cytokines stom effects. Peramivir can be used for the research of COVID-19 .
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-
- HY-170887
-
|
|
Keap1-Nrf2
Monoamine Oxidase
|
Inflammation/Immunology
|
|
MAO-B-IN-39 (compound11) is a selective monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-39 inhibits MAO-Bwith an IC50 of 3.61 μM. MAO-B-IN-39 demonstrates a potent NRF2 induction capacity. MAO-B-IN-39 exhibits potent anti-inflammatory and neuroprotective activity in OS (oxidative stress)-related in vitro models. MAO-B-IN-39 demonstrates high liver microsomal stability and favorable pharmacokinetics in mice. MAO-B-IN-39 is potential for Parkinson’s disease (PD) research .
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- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
- HY-182895
-
|
|
Influenza Virus
|
Infection
|
|
Influenza A virus-IN-19 (Compound (S)-63) is an orally active, selective Influenza A virus inhibitor with an EC50 of 0.44 μM. Influenza A virus-IN-19 exhibits moderate binding affinity to Hemagglutinin, with a Kd of 5.66 μM. Influenza A virus-IN-19 inhibits trypsin-mediated cleavage of HA0, blocks the early viral entry process, and suppresses the replication of Influenza A virus. Influenza A virus-IN-19 improves the survival rate of mice in lethal influenza models. Influenza A virus-IN-19 can be used in studies related to Influenza A virus infection .
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-
- HY-178015
-
|
|
Thyroid Hormone Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. THR-β agonist 11 shows potent cholesterol-lowering activity in cholesterol-fed rats. THR-β agonist 11 significantly reduces serum total TG, LDL-cholesterol, liver total TC and TG levels, and alleviates hepatic steatosis, inflammation and fibrosis in HFD-CCl4-induced Metabolic dysfunction-associated steatohepatitis (MASH) model mice. THR-β agonist 11 can be used for the study of metabolic dysfunction-associated steatohepatitis (MASH) and other fibrotic diseases .
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-
- HY-161953
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC50=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects .
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-
- HY-18099
-
S1RA
3 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
|
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
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-
- HY-155199
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD .
|
-
- HY-13241A
-
|
LY2228820
|
p38 MAPK
Autophagy
|
Cancer
|
|
Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
|
-
- HY-116330A
-
|
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
Cancer
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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-
- HY-183325
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
CXCR
TNF Receptor
|
Neurological Disease
|
|
FTO-IN-17 is an orally active and brain-penetrant FTO (m6A RNA demethylase) inhibitor with an IC50 of 1.1 μM. FTO-IN-17 stably binds the FTO catalytic pocket. FTO-IN-17 protects against Aβ1-42-induced toxicity while increasing global m6A levels and dampening pro-inflammatory gene (CXCL10, TNF-α) expression. FTO-IN-17 ameliorates anxiety-like behavior and rescues hippocampal-dependent spatial, recognition memory and neuroinflammation in Alzheimer's disease mice models .
|
-
- HY-117599
-
|
|
Parasite
|
Infection
|
|
JPC-3210 is an orally active aminomethylphenol. JPC-3210 exhibits anti-malarial activity with a mean IC50 ranging from 2.5 to 19 nM. JPC-3210 works by inhibiting the hemoglobin digestion pathway and promoting regulators of protein translation. JPC-3210 can inhibit CYP2D6 and CYP3A4 isozymes. JPC-3210 suppresses P. berghei infection in mice model. JPC-3210 possesses prophylactic protection in vivo. JPC-3210 can be studied in research on malaria prevention .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
-
- HY-P990117
-
|
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
- HY-P11297
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
AC-SDKP-NH2 is a substrate peptide of Angiotensin converting enzyme (ACE). AC-SDKP-NH2 has anti-inflammatory and anti-fibrotic activities. AC-SDKP-NH2 directly acts on tissues and prevents or reverses them from excessive fibrosis, but fails to reduce blood pressure and left ventricular hypertrophy (LVH). AC-SDKP-NH2 attenuates inflammation and cell differentiation, proliferation and migration, therefore reducing fibrosis in the heart, vessels and kidneys in mice model. AC-SDKP-NH2 can be used for cardiovascular diseases such as hypertension research .
|
-
- HY-174850
-
|
|
Btk
|
Cancer
|
|
CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
|
-
- HY-181647
-
|
|
Bacterial
Elastase
|
Infection
|
|
LasB-IN-3 is a protease elastase (LasB) inhibitor of Pseudomonas aeruginosa with an IC50 value of 8.5 nM. LasB-IN-3 shows an IC50 of 58.9 nM for the Met128Val mutant. LasB-IN-3 binds to active sites of wild-type and Met128Val mutant LasB, coordinates zinc ions, forms hydrogen bonds and CH-π interactions, and inhibits LasB proteolytic activity. LasB-IN-3 increases survival rate in LasB-induced acute lung injury mice models. LasB-IN-3 can be used for the research of Pseudomonas aeruginosa infection .
|
-
- HY-P5912
-
|
|
iGluR
Calcium Channel
|
Neurological Disease
|
|
GluN1 (356-385) is a polypeptide targeting NMDAR GluN1. GluN1 (356-385) induces the production of autoantibodies, which reduce the density of cell surface NMDAR clusters, impair long-term potentiation, and decrease NMDAR-mediated Ca 2+ influx. As an immunogen, GluN1 (356-385) induces symptoms similar to anti-NMDAR encephalitis, including memory loss, in mice. GluN1 (356-385) can be used to establish a mouse model that mimics the pathogenesis of anti-NMDAR encephalitis. GluN1 (356-385) is applicable to research related to anti-NMDAR encephalitis .
|
-
- HY-W111581
-
|
Diethyldithiocarbamic acid copper salt
|
Apoptosis
Caspase
|
Cancer
|
|
Copper(II) diethyldithiocarbamate (Diethyldithiocarbamic acid copper salt) is a Copper(II) and diethyldithiocarbamate coordination polymer. Copper(II) diethyldithiocarbamate binds tightly to NPL4 and induces its aggregation, disrupting the p97-NPL4-UFD1 pathway. Copper(II) diethyldithiocarbamate causes ubiquitinated proteins accumulation and impairs waste proteins degradation, thus resulting in cell apoptosis. Copper(II) diethyldithiocarbamate inhibits tumor growth in MDA-MB-231 xenograft mice models. Copper(II) diethyldithiocarbamate can be used for the research of cancer, such as breast cancer .
|
-
- HY-172883
-
|
|
FABP
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65 μM and 1.08 μM for FABP1 and FABP4, EC50 s of 9.19 μM, 2.20 μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
|
-
- HY-125726
-
|
(3'-sulfo)Galβ-Cer(d18:1/24:1); N-Nervonoyl Sulfatide; C24:1 Sulfatide
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
Sulfo galactosylceramide (N-Nervonoyl Sulfatide; C24:1 Sulfatide) is a glycolipid and the major sulfolipid species in mature myelin. Sulfo galactosylceramide interacts with C-type lectins and immunoglobulin-like receptors, with the highest affinity for LMIR5. Sulfo galactosylceramide induces MCP-1 production by basophils but not mast cells, and increases NFAT activation via LMIR5. Sulfo galactosylceramide alleviates symptoms and improves survival in a mouse model of chronic relapsing-remitting experimental autoimmune encephalomyelitis (EAE), and reduces inflammatory lesions and the number of infiltrating mononuclear cells in the lumbar spinal cord of EAE mice.
|
-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-B0340
-
|
DM9384; DZL-221
|
nAChR
iGluR
mGluR
PKC
GABA Receptor
Calcium Channel
|
Neurological Disease
|
|
Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca 2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research .
|
-
- HY-N4107
-
|
|
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-N4107R
-
|
|
Reference Standards
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
- HY-100591R
-
|
|
Sirtuin
Reference Standards
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SirReal2 (Standard) is the analytical standard of SirReal2 (HY-100591). This product is intended for research and analytical applications. SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
|
-
- HY-19938
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
MTL-005 is a boron-containing radiosensitizer used in Boron Neutron Capture Therapy (BNCT). MTL-005 enriches the boron-10 isotope in tumor tissues, causing nuclear fission under thermal neutron irradiation, releasing high linear energy transfer (LET) α particles and lithium ions, which selectively destroy tumor cells while minimizing damage to surrounding normal tissues. MTL-005 significantly controlls the tumor progression in the SCCVII squamous cell carcinoma mouse model and prolonged the survival of the mice. MTL-005 can be used to study solid tumors such as head and neck cancer.
|
-
- HY-182288
-
|
|
STAT
Apoptosis
|
Cancer
|
|
YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer .
|
-
- HY-183710
-
|
|
CDK
Androgen Receptor
c-Myc
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer .
|
-
- HY-101117R
-
|
|
Histone Methyltransferase
Reference Standards
|
Cancer
|
|
EED226 (Standard) is the analytical standard of EED226 (HY-101117). This product is intended for research and analytical applications. EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
|
-
- HY-178738
-
|
|
Antibiotic
Bacterial
Topoisomerase
DNA/RNA Synthesis
|
Infection
|
|
GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis .
|
-
- HY-170970
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-10 (Compound P15) is a Rv1625c/Cya activator that regulates cAMP metabolism to influence the growth of Mycobacterium tuberculosis (Mtb). Mtb-IN-10 exhibits an EC50 of 1.96 µM in an Mtb-infected macrophage model and demonstrates 58.0% oral bioavailability in mice at a 20 mg/kg dose. It may regulate intracellular signaling and disrupt cholesterol metabolism in Mtb, thereby inhibiting bacterial proliferation. Mtb-IN-10 holds potential for tuberculosis (TB) research, particularly for combating multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) Mtb strains .
|
-
- HY-176224
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Anti-virulence factor-IN-2 (compound C7) is an inhibitor targeting the virulence factor KpsM in Escherichia coli. kpsM mediates the translocation of capsular polysaccharides to the cell surface, allowing kpsM-positive E. coli to escape the phagocytosis of the scavenger receptor Marco on liver Kupffer cells, leading to bacterial dissemination. kpsM-positive E. coli exacerbates ethanol-induced liver disease. Anti-virulence factor-IN-2 can inhibit the ethanol-induced liver disease model caused by kpsM-dependent capsid in mice and has anti-infective activity. Anti-virulence factor-IN-2 can be used for the study of alcoholic hepatitis .
|
-
- HY-17484R
-
|
CP 65703 (Standard)
|
Reference Standards
|
Inflammation/Immunology
|
|
Ampiroxicam (Standard) is the analytical standard of Ampiroxicam. This product is intended for research and analytical applications. Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases.
|
-
- HY-156792
-
|
|
RIO Kinase
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
|
-
- HY-P991590
-
|
|
MHC
Apoptosis
JNK
Reactive Oxygen Species (ROS)
|
Cancer
|
|
1D09C3 is a fully human anti-HLA-DR monoclonal antibody. 1D09C3 induces apoptosis and cell death involving a cascade of events, including ROS generation, JNK activation, mitochondrial membrane depolarization, and AIF release from mitochondria. 1D09C3 shows potent anti-tumor activity and increases overall survival and median survival in JVM-2 cells and GRANTA-519 cells xenograft mice models. 1D09C3 can be used for the researches of cancer, such as chronic lymphocytic leukemia (CLL) .
|
-
- HY-W020788
-
|
CGA 154281
|
Environmental Pollutants
Glutathione S-transferase
Estrogen Receptor/ERR
Pregnane X Receptor (PXR)
FXR
|
Metabolic Disease
Cancer
|
Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity .
|
-
- HY-176194
-
|
|
Collagen
c-Fms
PDGFR
Src
|
Inflammation/Immunology
|
|
Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model .
|
-
- HY-145774
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester proagent of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice .
|
-
- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
-
- HY-16561
-
-
- HY-114162B
-
|
SNDX-50469 mesylate
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
|
-
- HY-P991584
-
|
|
FGFR
|
Cancer
|
|
HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer .
|
-
- HY-A0042
-
|
CGP 33101; E 2080; RUF 331
|
Sodium Channel
|
Neurological Disease
|
|
Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
|
-
- HY-175478
-
|
|
Phosphodiesterase (PDE)
STING
|
Inflammation/Immunology
Cancer
|
|
Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity against ENPP2 and 10-fold selectivity against ENPP3. Enpp-1-IN-27 stabilizes cGAMP levels and activates the STING pathway, promoting cytokine release and enhancing innate immune responses. Enpp-1-IN-27 induces ISRE activation and amplified cGAMP-mediated immune responses and shows the desired antitumor efficacy in the 4T1 and CT26 syngeneic mouse models. Enpp-1-IN-27 can used for the studies of breast cancer and colon cancer .
|
-
- HY-P99118
-
|
HLX 10
|
PD-1/PD-L1
Akt
STAT
|
Cancer
|
|
Serplulimab (HLX 10) is a humanized anti-PD-1 monoclonal antibody. Serplulimab can inhibit tumor growth, regulate the tumor microenvironment, and has anti-tumor activity. Serplulimab can be used in the research of cancer such as lung cancer and colon cancer .
|
-
- HY-139901
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma .
|
-
- HY-19720A
-
|
ACU-4429 hydrochloride
|
RPE65
|
Metabolic Disease
|
|
Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD) .
|
-
- HY-P5128
-
|
Satoreotide tetraxetan
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
|
DOTA-JR11 is a somatostatin receptor 2 (SSTR2)antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research . DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-19720
-
|
ACU-4429
|
RPE65
|
Metabolic Disease
|
|
Emixustat is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD) .
|
-
- HY-P11634
-
|
|
Bacterial
|
Infection
|
|
KF-22 is an antimicrobial peptide that exhibits antimicrobial activity against both Gram-negative and Gram-positive bacteria. KF-22 demonstrates broad-spectrum, potent activity against multidrug-resistant bacteria with low toxicity. KF-22 can be used in research related to infections .
|
-
- HY-182304
-
|
|
Amyloid-β
α-synuclein
Amylin Receptor
Tau Protein
SOD
|
Neurological Disease
|
|
CLR01 sodium is a blood-brain barrier-permeable anti-aggregation agent. CLR01 sodium inhibits the de novo aggregation of Amyloid-β 40/42, α-synuclein, IAPP, tau protein and SOD1. CLR01 sodium reduces amyloid plaque burden in the cortex of triple-transgenic mice and improves the memory and motor abilities of these mice. CLR01 sodium can be used in research related to Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS) .
|
-
- HY-177021
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-51 is an orally available, potent tubulin inhibitor (IC50 = 31 nM). Tubulin-IN-51 promotes tubulin polymerization in vitro and does not compete with Paclitaxel (HY-B0015) for binding. Tubulin-IN-51 inhibits the binding of Vinblastine (HY-13780) to tubulin. Tubulin-IN-51 downregulates the proportion of cells in the G1 phase and induces apoptosis. Tubulin-IN-51 inhibits tumor growth in multiple nude mouse xenograft models .
|
-
- HY-P991243
-
|
|
EGFR
Akt
|
Cancer
|
|
MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
|
-
- HY-172930
-
|
|
Molecular Glues
IKZF Family
Potassium Channel
|
Inflammation/Immunology
Cancer
|
|
PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
|
-
- HY-16561R
-
|
trans-Resveratrol (Standard); SRT501 (Standard)
|
Reference Standards
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-181136
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Antiestrogenic agent-1, an organophosphorus 13α-estrone derivative, is an antiestrogenic agent. Antiestrogenic agent-1 can disrupt estrogen signaling by inhibiting estrogen-mediated transcriptional activity. Antiestrogenic agent-1 can inhibit cancer cells proliferation, migration, invasion and induce G1-phase arrest. Antiestrogenic agent-1 mitigates estrogen-induced uterine growth in immature rats and inhibits tumor growth in a murine triple-negative breast cancer mice model. Antiestrogenic agent-1 can be used for the researches of cancer and endocrinology,such as breast cancer, oropharyngeal squamous cell carcinoma .
|
-
- HY-178016
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy .
|
-
- HY-16561S1
-
|
trans-Resveratrol-13C6; SRT501-13C6
|
Isotope-Labeled Compounds
DNA/RNA Synthesis
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-123882
-
|
|
Endogenous Metabolite
|
Others
|
|
IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
|
-
- HY-P5396A
-
|
|
Amino Acid Decarboxylase
|
Others
|
|
GAD65 (524-543) acetate is a biological active peptide with amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). GAD65 (524-543) acetate is one of the first fragments of the islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. GAD65 (524-543) acetate is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with GAD65 (524-543) acetate increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells .
|
-
- HY-169059
-
|
|
Ferroptosis
|
Inflammation/Immunology
|
|
Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
|
-
- HY-W009123
-
|
cis-13-Docosenamide
|
Endogenous Metabolite
Bacterial
|
Infection
Neurological Disease
|
|
Erucamide is an orally active, blood-brain barrier-permeable TMEM19 ligand and T3SS inhibitor. Erucamide exerts retinal neuroprotective effects in mouse models of retinal degeneration. Erucamide attenuates depression- and anxiety-like behaviors in mice.\n\nErucamide binds to the conserved hydrophobic pocket in HrcC, disrupts its outer membrane localization, and blocks T3SS-mediated effector protein secretion in Gram-negative pathogenic bacteria. Erucamide enhances the antimicrobial immunity of plants against pathogenic bacteria. Erucamide can be used in research related to retinitis pigmentosa, anxiety and depression, bacterial wilt, and bacterial blight .
|
-
- HY-P11287
-
|
|
Interleukin Related
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
DOTA-Pep-1L is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L can be used for PET imaging, tumor targeting and glioma research .
|
-
- HY-116330
-
|
|
Calcium Channel
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
|
-
- HY-186105
-
|
|
NAMPT
|
Neurological Disease
|
|
P7C3-S243 is a brain-penetrant P7C3 class of neuroprotective agent. P7C3-S243 augments synthesis of nicotinamide adenine dinucleotide through activation of the metabolic enzyme nicotinamide phosphoribosyltransferase. P7C3-S243 shows potent neuroprotective efficacy in parkinson’s disease mice models. P7C3-S243 can be used for the research of parkinson’s disease .
|
-
- HY-175670
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .
|
-
- HY-181752
-
|
|
FGFR
TNK1
Apoptosis
Caspase
|
Cancer
|
|
FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC50 of 6.8 nM. FGFR3-IN-12 shows an IC50 of 19.2 nM against FGFR3 V555M and an IC50 of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer .
|
-
- HY-16561S
-
|
trans-Resveratrol-d4; SRT501-d4
|
Isotope-Labeled Compounds
DNA/RNA Synthesis
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-168166
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .
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- HY-169135
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PROTACs
Proteasome
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Cancer
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|
PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader for 20S proteasome subunit β5, with a DC50 of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 inhibits the proliferation of cancer cell FaDu with IC50 of 0.23 μM. PROTAC 20S proteasome subunit β5 degrader 2 exhibits antitumor efficacy in mice models . (Pink: Ligand for target protein (HY-10227); Blue: Ligand for E3 ligase (HY-103596); Black: Linker (HY-Y1760))
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- HY-P5396
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Amino Acid Decarboxylase
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Others
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GAD65 (524-543) is a biological active peptide with amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). GAD65 (524-543) is one of the first fragments of islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. GAD65 (524-543) is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with GAD65 (524-543) increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells .
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- HY-16639
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GPR35
Neurotensin Receptor
|
Neurological Disease
Endocrinology
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ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
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- HY-P10786
-
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Transmembrane Glycoprotein
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Cancer
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LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
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- HY-182802
-
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Ferroptosis
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
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Cancer
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Ferroptosis inducer-15 is a ferroptosis inducer. Ferroptosis inducer-15 downregulates GPX4 expression, triggers lipid peroxidation via ROS accumulation, and disrupts mitochondrial membrane potential to drive ferroptosis. Ferroptosis inducer-15 increases splenic CD4 + T cell proportion, promotes CD8 + cytotoxic T cell tumor infiltration, and activates antitumor immune responses. Ferroptosis inducer-15 exerts antiproliferative activity against colorectal cancer cells and inhibits tumor growth in xenograft mice models without significant body weight loss. Ferroptosis inducer-15 can be used for the research of cancer, such as colorectal cancer .
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- HY-171572
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Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
Apoptosis
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Inflammation/Immunology
Cancer
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Atezolizumab-MMAE is an anti-PD-L1 antibody-drug conjugate (ADC) with an EC50 of 1.1 nM. Atezolizumab-MMAE is composed of a humanized anti-PD-L1 antibody (Atezolizumab) (HY-P9904), a lysosomally cleavable dipeptide linker (valine-citrulline), a tubulin inhibitor (MMAE) (HY-15162), and the drug-linker conjugate for ADC is VcMMAE (HY-15575). Atezolizumab-MMAE has a potent cytotoxicity (EC50: 9.75-11.94 nM) and immune activation effect. Atezolizumab-MMAE has a significantly anti-tumor activity in MC38 xenograft PD-1-humanized immune system mice model .
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- HY-W011168
-
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Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
|
Inflammation/Immunology
Cancer
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8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
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- HY-P6292
-
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PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
|
Neurological Disease
Cancer
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KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
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- HY-173428
-
|
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Fungal
|
Infection
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|
Antifungal agent 130 (Compound A7) is an orally active antifungal agent. Antifungal agent 130 has good antifungal activity against Candida albicans (MIC = 0.12 ng/mL) and Cryptococcus neoformans (MIC = 0.12 ng/mL) and has excellent antivirulence effect. Antifungal agent 130 exerts its antifungal effect by disrupting the iron homeostasis of fungal cells and inducing oxidative stress damage. Antifungal agent 130 can inhibit the formation of fungal virulence factors (such as biofilm, capsule, urease and melanin). Antifungal agent 130 has good antifungal effect and can be used in the study of drug-resistant fungal infections .
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-
- HY-174212
-
|
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Apoptosis
|
Cancer
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MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.
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- HY-N2345
-
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Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
|
Inflammation/Immunology
Cancer
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Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .
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- HY-N2345R
-
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Reference Standards
Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
|
Inflammation/Immunology
Cancer
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Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .
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-
- HY-110195
-
-
- HY-B0869
-
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Acetolactate Synthase (ALS)
Herbicide
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Others
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|
Bispyribac is an acetolactate synthase inhibitor that can be used as a systemic post-emergence herbicide for control of weeds in agriculture. Bispyribac blocks the amino acid synthesis. Bispyribac has low acute toxicity in animal models .
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- HY-146223
-
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Ras
p38 MAPK
PI3K
Apoptosis
|
Cancer
|
|
AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
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- HY-159124
-
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Sirtuin
|
Cancer
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|
YZL-51N is a selective SIRT7 inhibitor with IC50 value of 12.71 μM. YZL-51N disrupts SIRT7 enzyme activity by occupying the NAD + binding pocket, thereby weakening DNA damage repair and inhibiting cancer cell survival. YZL-51N possesses anti-tumor activity and can be used in cancer research .
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- HY-P11287A
-
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Interleukin Related
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
DOTA-Pep-1L TFA is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L TFA specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L TFA yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L TFA can be used for PET imaging, tumor targeting and glioma research .
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- HY-W017540
-
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ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
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Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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- HY-W338346
-
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Drug Derivative
Interleukin Related
TNF Receptor
Polo-like Kinase (PLK)
|
Inflammation/Immunology
Cancer
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Salicylate choline is an orally active derivative of Aspirin (acetylsalicylic acid) (HY-14654). Salicylate choline significantly reduces IL-1β, IL-6, TNF-α and IL-10 levels in cells. Salicylate choline enhances the anti-tumor activity of the CRM1 inhibitor Selinexor (KPT-330) (HY-17536) through inducing S-phase cell cycle arrest and impairing DNA damage repair. Salicylate choline combined with Selinexor demonstrates excellent anti-tumor efficacy in mice xenograft model harboring JeKo-1 cells. Salicylate choline can be used for the study of rheumatic diseases, inflammation and cancer .
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- HY-W142432
-
|
|
Biochemical Assay Reagents
β-catenin
Wnt
Arginase
TGF-beta/Smad
mTOR
Akt
ERK
Atg8/LC3
p62
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
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-
- HY-148273
-
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ASP-3082; KRAS G12D inhibitor 17
|
PROTACs
Ras
ERK
Akt
|
Cancer
|
|
Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .
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-
- HY-159898
-
-
- HY-148640
-
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BCL6
MDM-2/p53
Histone Methyltransferase
CXCR
Apoptosis
|
Cancer
|
|
WK500B is a potent and orally active BCL6 inhibitor with a KD of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL) .
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-
- HY-P11582
-
|
|
Bacterial
|
Infection
|
|
CyLip-20 is a cyclic lipopeptide antimicrobial peptide that targets Gram-positive and Gram-negative bacteria. CyLip-20 exhibits low hemolytic activity and mild in vivo toxicity. CyLip-20 disrupts the integrity of bacterial outer membrane, inner membrane and cytoplasmic membrane by binding to bacterial lipopolysaccharide (LPS), triggering membrane permeabilization, depolarization and leakage of intracellular contents, and inhibits bacterial biofilm formation. In animal models, CyLip-20 reduces the bacterial load in skin wounds of mice infected with MRSA, promotes wound healing, decreases the levels of inflammatory cytokines and reduces inflammatory cell infiltration. CyLip-20 can be used in research related to MRSA skin wound infections .
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- HY-116330AR
-
|
Hyperforin DCHA (Standard)
|
Reference Standards
TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin dicyclohexylammonium salt (Standard) is the analytical standard of Hyperforin dicyclohexylammonium salt. This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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-
- HY-169177
-
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JNK
|
Inflammation/Immunology
|
|
JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
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-
- HY-W017540R
-
|
|
Reference Standards
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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-
- HY-B1451
-
|
TA-6366
|
Angiotensin-converting Enzyme (ACE)
MMP
JNK
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions .
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- HY-181839
-
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Discoidin Domain Receptor
|
Inflammation/Immunology
|
|
DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis .
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-
- HY-153068
-
-
- HY-P990215
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Anti-Mouse IL-27 p28 Antibody (MM27.7B1) is a mouse-derived anti-mouse IL-27 p28 IgG2a, κ type antibody inhibitor. Anti-Mouse IL-27 p28 Antibody (MM27.7B1) can neutralize IL-27. Anti-Mouse IL-27 p28 Antibody (MM27.7B1) delays CD8+ T cell reconstitution mediated by IL-27 after murine anti-thymocyte globulin (mATG) treatment in BALB/c heart allografts mice models .
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-
- HY-123929
-
|
|
MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
|
Cancer
|
|
PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
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-
- HY-119024
-
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SHP1
STAT
|
Cancer
|
|
BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8 + T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields .
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-
- HY-W663179
-
|
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Parasite
Cytochrome P450
|
Infection
|
|
DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .
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-
- HY-W020788R
-
|
CGA 154281 (Standard)
|
Reference Standards
Glutathione S-transferase
Estrogen Receptor/ERR
Pregnane X Receptor (PXR)
FXR
|
Others
|
|
Benoxacor (Standard) is the analytical standard of Benoxacor. This product is intended for research and analytical applications. Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity .
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-
- HY-176128
-
|
|
PROTACs
Androgen Receptor
Apoptosis
PARP
Caspase
|
Cancer
|
|
BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .
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-
- HY-182014
-
|
|
LXR
|
Cardiovascular Disease
Metabolic Disease
|
|
TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRα and LXRβ, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRα/β transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders .
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- HY-W088065
-
|
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Environmental Pollutants
DNA/RNA Synthesis
|
Others
|
Sodium formate acts as a key promoter for heterogeneous nucleation of ZIF crystals and thin film synthesis. It is also recognized as a GRAS substance by the FDA, and serves as a cosmetic preservative and food additive. Sodium formate has low acute oral toxicity (acute oral LD50=7410 mg/kg and acute intravenous LD50=807 mg/kg in mice), with no heritable or carcinogenic effects, but exhibits embryonic developmental toxicity and teratogenicity at high concentrations. Sodium formate may cause moderate irritation to rabbit eyes, is relatively safe to the skin, and does not induce tumor formation in rats in vivo. Sodium formate is rapidly absorbed and oxidized to carbon dioxide in vivo, and forms DNA adducts in specific metabolic deficiency models or upon high-dose exposure .
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-
- HY-176180
-
|
|
PROTACs
STING
NF-κB
IKK
|
Inflammation/Immunology
|
|
PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC50 of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model . Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181
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-
- HY-118243
-
|
|
Amyloid-β
|
Others
|
|
KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
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-
- HY-173522
-
|
|
Kinesin
Microtubule/Tubulin
|
Cancer
|
|
KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (Ex/Em = 410/510 nm). KIF2C-IN-1 exhibits notable cytotoxicity and weak inhibitory effects on KIF2A/B. KIF2C-IN-1 prohibits the dissociation of KIF2C from microtubules. KIF2C-IN-1 inhibiting KIF2C reverses cross-resistance to microtubule-targeting agents. KIF2C-IN-1 reduces tumorigenesis in chemoresistant triple-negative breast cancer (TNBC) model in mice with the combination of Paclitaxel (HY-B0015) .
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-
- HY-167939
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
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-
- HY-N0976
-
|
11b-Hydroxy-11b,1-dihydromedicarpin
|
Interleukin Related
Wnt
|
Inflammation/Immunology
|
|
1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative . Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
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-
- HY-126969
-
|
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PPAR
|
Metabolic Disease
|
|
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
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-
- HY-172883A
-
|
|
FABP
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
(E/Z)-ABP/PPAR modulator 1 is a mixture of the E and Z isomers of ABP/PPAR modulator 1 (HY-172883). ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65 μM and 1.08 μM for FABP1 and FABP4, EC50 s of 9.19 μM, 2.20 μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
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-
- HY-16561G
-
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trans-Resveratrol; SRT501
|
DNA/RNA Synthesis
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-P10792
-
|
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EGFR
|
Cancer
|
|
HER2-targeted peptide H6F is a HER2 targeting peptide that binds to HER2 to target breast cancer cells, with the amino acid sequence YLFFVFER. The HER2-targeted peptide H6F can be conjugated with the bifunctional chelating agent hydrazinonicotinamide (HYNIC) for radiolabeling with 99mTc. Single-photon emission computed tomography (SPECT) imaging shows that the labeled HER2-targeted peptide H6F specifically accumulates in HER2-positive MDA-MBA-453 tumor-bearing mice models. The HER2-targeted peptide H6F can be used for tumor molecular imaging studies .
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-
- HY-145836
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
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-
- HY-N0538
-
|
Xylite
|
Environmental Pollutants
Endogenous Metabolite
Bacterial
Autophagy
Atg7
Atg8/LC3
|
Metabolic Disease
Cancer
|
|
Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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-
- HY-128574
-
|
DS11252927
|
GLUT
PI3K
Akt
|
Metabolic Disease
|
|
D927 (DS11252927) is an orally active glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM. D927 enhances the binding affinity of PI3Kα catalytic subunit p110α to canonical RAS proteins (KRAS4A, KRAS4B) and RRAS, RRAS2, MRAS. D927 activates the PI3Kα-AKT pathway (increasing phosphorylation of AKT, p70S6 kinase) without affecting the RAF-ERK1/2 pathway. D927 improves hyperglycemia in type 1 and type 2 diabetes mice model. D927 can be used for the study of glucose homeostasis disorders and diabetes .
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-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
|
-
- HY-P992074
-
|
IPH6501
|
CD20
Interleukin Related
|
Cancer
|
|
Zemlikafusp alfa (IPH6501) is a tetra-specific NK cell engager that targets CD20, CD16a, NKp46 and carries an IL-2 variant. Zemlikafusp alfa (IPH6501) is used in research for the treatment of relapsed/refractory B-cell non-Hodgkin lymphoma .
|
-
- HY-172795
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
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-
- HY-N2736
-
|
|
Beta-lactamase
COX
Interleukin Related
Bacterial
JNK
ERK
p38 MAPK
STAT
Apoptosis
NO Synthase
Nuclear Factor of activated T Cells (NFAT)
Lactate Dehydrogenase
Reactive Oxygen Species (ROS)
SOD
Akt
Caspase
Bcl-2 Family
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
3′,4′,7-Trihydroxyflavone is an orally active inhibitor of OXA-48 (IC50 = 1.89 μM) and COX-1 (IC50 = 36.37 μM). 3′,4′,7-Trihydroxyflavone exhibits antioxidant and anti-inflammatory properties, inhibiting the release of inflammatory cytokines such as IL-6, IL-8, and TNF-α. 3′,4′,7-Trihydroxyflavone inhibits H2O2-induced neuronal apoptosis and ROS accumulation, and exerts anti-neuroinflammatory effects by suppressing the JNK-STAT1 pathway. 3′,4′,7-Trihydroxyflavone exhibits antimicrobial and antibiotic-modifying activities against multidrug-resistant Gram-negative enteric bacteria. 3′,4′,7-Trihydroxyflavone inhibits RANKL-induced osteoclast formation via NFATc1. 3′,4′,7-Trihydroxyflavone activates the CREB-BDNF axis and restores scopolamine (HY-N0296)-induced memory deficits in mice .
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-
- HY-175785
-
|
|
Estrogen Receptor/ERR
Aryl Hydrocarbon Receptor
Apoptosis
MDM-2/p53
|
Cancer
|
|
X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .
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-
- HY-N6257
-
-
- HY-175326
-
|
|
SOS1
|
Cancer
|
|
SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
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-
- HY-181306
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC EZH2 Degrader-11 (compound 2) is a EZH2-targeting PROTAC protein degrader. PROTAC EZH2 Degrader-11 reduces tumor size and viability in 3D spheroid models. PROTAC EZH2 Degrader-11 can be used for the research of cancer .
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-
- HY-19796
-
|
Aramchol; C20-FABAC
|
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
|
|
Icomidocholic acid (Aramchol) is a lipid molecule synthesized from cholic acid and arachidic acid. Icomidocholic acid is an orally active SCD1 inhibitor and cholesterol solubilizer with antifibrotic effects. Icomidocholic acid can reduce liver fat content, dissolve cholesterol crystals and prevent gallstone formation. Icomidocholic acid can be used in the study of nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) .
|
-
- HY-156483
-
TT-012
2 Publications Verification
|
Microphthalmia Associated Transcription Factor (MITF)
|
Cancer
|
|
TT-012 is a MITF inhibitor with a human MITF IC50 of 13.1 nM and a human MITF Kd value of 15.5 nM. TT-012 reduces mRNA levels of MITF downstream genes linked to melanosome biogenesis, cell survival, and proliferation, and upregulates cell cycle-inhibiting genes. TT-012 can be used for the research of melanoma[1][2][3].
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-
- HY-181739
-
|
|
CD1
|
Cancer
|
|
GCB-27a is a CD1d-binding immunostimulant and antitumor agent. GCB-27a binds to CD1d to form a stable complex and presents it to NKT cells, enhancing hydrophobic interactions within the A' pocket of CD1d through branched-chain conformation restriction. GCB-27a induces a Th1-biased immune response, drives IFN−γ production and limits IL-4 levels. GCB-27a is applicable to research related to melanoma lung metastasis .
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-
- HY-P991958
-
|
|
CTLA-4
|
Cancer
|
|
GIGA-564 is a fully human anti-CTLA4 IgG1 monoclonal antibody with a Kd of 9.8 nM. GIGA-564 binds to a unique epitope of CTLA-4, mediates FcR-dependent signaling pathways, depletes CTLA-4-highly-expressing regulatory T cells within tumors, and inhibits the proliferation of peripheral regulatory T cells. GIGA-564 exhibits anti-tumor activity in mouse models. GIGA-564 can be used for tumor research .
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- HY-172903
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Nav1.8-IN-16 (Compound (R)-40) is an orally active and selective hNaV 1.8 inhibitor (IC50: 5.9 nM). Nav1.8-IN-16 exerts analgesic effects by blocking NaV1.8 channels without significantly affecting other NaV subtypes or hERG channels. Nav1.8-IN-16 exhibits dose-dependent analgesic effects in postoperative pain and inflammatory pain models and can be used in pain-related research .
|
-
- HY-182712
-
|
|
Glycosidase
|
Cancer
|
|
HPSE-IN-2 is a heparanase (HPSE) inhibitor with an IC50 of 0.27 µM. HPSE-IN-2 reduces lung metastasis in mouse models. HPSE-IN-2 can be used for the research of melanoma .
|
-
- HY-173290
-
|
|
Phosphodiesterase (PDE)
Interleukin Related
CXCR
TNF Receptor
|
Inflammation/Immunology
|
|
PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis .
|
-
- HY-144658
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
|
-
- HY-181123
-
|
|
COX
|
Neurological Disease
Inflammation/Immunology
|
|
AS1-6 is a selective COX-2 inhibitor with an IC50 of 2.7 μM. AS1-6 has an IC50 of 12.6 μM for COX-1. AS1-6 exerts significant anti-inflammatory and analgesic activities. AS1-6 can be used in research on non-steroidal anti-inflammatory agents .
|
-
- HY-N16465
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
STAT
|
Inflammation/Immunology
|
|
Cinnamtannin D1 is an orally active polyphenolic compound with immunosuppressive activity. Cinnamtannin D1 regulates the balance of Th17/Treg cells by inhibiting AHR expression. Cinnamtannin D1 reduces apoptosis and ROS in INS-1 cells and primary cultured murine islets induced by Palmitic acid (PA) (HY-N0830). Cinnamtannin D1 reduces Th17 cell differentiation via downregulating p-STAT3/RORγt and promotes Treg cell differentiation via upregulating p-STAT5/Foxp3. Cinnamtannin D1 exerts excellent anti-arthritic efficacy in collagen-induced arthritis (CIA) model of mice. Cinnamtannin D1 can be used for the study of rheumatoid arthritis (RA) .
|
-
- HY-W587414
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Neospiramycin I is a macrolide antibiotic and a derivative of Spiramycin I (HY-N7141). Neospiramycin I is effective against the macrolide-sensitive KB210 strain of S. aureus, but ineffective against the macrolide-resistant KB224 strain, with minimum inhibitory concentrations (MIC) of 3.12 and greater than 100 µg/mL, respectively; it is also effective against B. cereus, B. subtilis, M. luteus, E. coli, and K. pneumoniae, with respective MIC values of 1.56, 3.12, 3.12, 0.2, 50, and 12.5 µg/mL. Neospiramycin I binds to the ribosomes of E. coli, with an inhibitory concentration 50 (IC50) of 1.2 µM. It protects mice from death in a type III S. pneumoniae infection model, with an effective dose 50 (ED50) of 399.8 mg/kg .
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-
- HY-W017540S
-
|
|
Isotope-Labeled Compounds
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Cyclocreatine- 13C3 is the 13C-labeled Cyclocreatine (HY-W017540). Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
|
-
- HY-N6893
-
|
|
NF-κB
NOD-like Receptor (NLR)
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
Ergolide is an orally active dual inhibitor targeting NF-κB/p65 and NLRP3. Ergolide blocks the NF-κB signaling pathway and the nuclear translocation of p65, and irreversibly binds to the NACHT domain of NLRP3 to inhibit inflammasome assembly. Ergolide significantly reduces the production of inflammatory mediators (e.g., NO, PGE2) and cytokines, induces cancer cell apoptosis, autophagy and ROS generation. Ergolide also enhances the anti-tumor effect of vincristine. Ergolide alleviates acute lung injury via an NLRP3-dependent mechanism, and effectively improves the survival rate and behavioral function of septic mice and inflammatory zebrafish models. Ergolide is used in the research of metastatic uveal melanoma, neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease), sepsis and acute lymphoblastic leukemia .
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-
- HY-169478
-
|
|
Liposome
|
Cancer
|
|
Lipid N2-3L is an ionizable cationic lipid (pKa = 8.99) that can be used to generate supramolecular lipid nanoparticles (SMLNPs) for mRNA delivery. Lipid nanoparticles formed by encapsulating a luciferase reporter gene with Lipid N2-3L were detected to accumulate in the lymph nodes of mice, indicating that they can effectively enter the mouse immune system. Lipid nanoparticles formed by encapsulating ovalbumin mRNA and the TLR7/8 agonist Resiquimod (HY-13740) with Lipid N2-3L were able to reduce tumor volume and increase survival in the MC-38-OVA mouse colon cancer model. Lipid N2-3L can be used in the research of drug delivery for cancer-related therapies .
|
-
- HY-159905
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy .
|
-
- HY-172158
-
|
|
Anaplastic lymphoma kinase (ALK)
Caspase
|
Cancer
|
|
ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m 6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia .
|
-
- HY-183327
-
|
|
PI3K
mTOR
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Bcl-2 Family
Caspase
|
Cancer
|
|
PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC50 values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models .
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-
- HY-W142432S
-
|
|
Isotope-Labeled Compounds
Biochemical Assay Reagents
β-catenin
Wnt
Arginase
TGF-beta/Smad
mTOR
Akt
ERK
Atg8/LC3
p62
Autophagy
|
Metabolic Disease
|
|
Perfluoroundecanoic acid- 13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
|
-
- HY-D3186
-
|
|
Fluorescent Dye
Glycosidase
|
Cancer
|
|
HMRef-βGal is a fluorescent probe and a substrate responsive to β-galactosidase (β-galactosidase) (Ex/Em=498 nm/505-600 nm). After being cleaved by β-galactosidase, HMRef-βGal triggers significant fluorescence enhancement via intramolecular spirocyclic function regulation. HMRef-βGal generates bright fluorescence in cancer cells with elevated β-galactosidase activity, enabling visualization of tiny peritoneal metastases in mouse models. HMRef-βGal exhibits low in vitro cytotoxicity and low acute in vivo toxicity in mice. HMRef-βGal can be used for preclinical fluorescence-guided diagnosis and cytoreductive surgery of peritoneal metastases, including compatibility with real-time naked-eye detection and endoscopic imaging, as well as for studies related to peritoneal metastases of ovarian cancer .
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-
- HY-143792
-
|
|
Huntingtin
P-glycoprotein
|
Neurological Disease
|
|
HTT-D3 is an orally active, blood-brain barrier penetrant splicing modulator of huntingtin (HTT). HTT-D3 promotes the inclusion of a pseudo-exon containing a premature termination codon into HTT pre-mRNA, triggers nonsense-mediated mRNA degradation and reduces HTT protein levels. HTT-D3 induces dose-dependent, comparable reductions in mutant HTT protein in both the brain and peripheral tissues of transgenic mouse models. HTT-D3 can be used for the research of Huntington's disease .
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-
- HY-176288
-
|
|
Eukaryotic Initiation Factor (eIF)
Bcl-2 Family
Apoptosis
Ras
PERK
|
Cancer
|
|
eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice .
|
-
- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-163027
-
|
|
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research .
|
-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
Metabolic Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-175320
-
|
|
PROTACs
c-Met/HGFR
Apoptosis
STAT
|
Cancer
|
|
PROTAC c-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader with DC50s of 0.42 and 0.32 nM in EBC-1 and Hs746T cells, respectively. PROTAC c-Met degrader-5 significantly induces cell apoptosis, G1 cell cycle arrest, and inhibits cell migration and invasion. PROTAC c-Met degrader-5 has potent antiproliferative and degradation efficacy against c-Met-addicted cancer cells and Tepotinib (HY-14721)-resistant cancer cells . Pink: c-Met ligand (HY-W425461); Blue: CRBN ligase ligand (HY-14658); Black: linker
|
-
- HY-W767399
-
|
|
Isotope-Labeled Compounds
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
8-Bromo-2'-deoxyguanosine- 13C, 15N2 is the 13C- and 15N-labeled 8-Bromo-2'-deoxyguanosine (HY-W011168). 8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
|
-
- HY-181779
-
|
|
Bacterial
|
Infection
|
|
Pyridomycin-4-F, Pyridomycin (HY-111402) derivative, is an antimycobacterial agent targeting fatty acid synthesis enzyme InhA (enoyl ACP reductase). Pyridomycin-4-F binds to the pyridomycin binding pocket of InhA, forms hydrogen bond interactions with Lys-165. Pyridomycin-4-F can be used for the research of tuberculosis .
|
-
- HY-D3220
-
|
|
Fluorescent Dye
Amyloid-β
|
Neurological Disease
|
|
PTO-41 is a blood-brain barrier-permeable near-infrared fluorescent probe that targets β-amyloid oligomers (Aβ Oligomers, AβOs) with a Kd of 349 nM. PTO-41 exhibits low cytotoxicity, high sensitivity to β-amyloid oligomers in in vitro phantom imaging, and can be rapidly cleared from the brain. PTO-41 is applicable to the research of Alzheimer's disease (Ex/Em = 538 nM/680 nM) .
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- HY-178163
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Ferroptosis
Necroptosis
RIP kinase
Reactive Oxygen Species (ROS)
Mixed Lineage Kinase
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Inflammation/Immunology
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Zharp1-163 is a dual inhibitor of ferroptosis and necroptosis. Zharp1-163 effectively blocks ferroptosis by reducing reactive oxygen species (ROS) levels and inhibits necroptosis by potently and selectively targeting RIPK1 kinase activity (KD = 240 nM; IC50 = 406.1 nM). Zharp1-163 inhibits the cellular activation of RIPK1, RIPK3 and MLKL in response to necroptotic stimulation. Zharp1-163 markedly attenuates TNF-α (HY-P1875)-induced systemic inflammatory syndrome, including the prevention of TNF-α-induced mortality and hypothermia in mice. Zharp1-163 significantly alleviates acute kidney injury associated with both necroptosis and ferroptosis in models induced by Cisplatin (HY-17394) and ischemia-reperfusion. Zharp1-163 can be used for the study of diseases associated with cell death pathways, such as kidney disease .
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- HY-113308
-
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Calcium Channel
Ferroptosis
PI3K
Akt
HBV
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis (Ferroptosis), viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-W768347
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Xylite-13C5
|
Isotope-Labeled Compounds
Bacterial
Autophagy
Endogenous Metabolite
Atg8/LC3
Atg7
|
Cancer
|
|
Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-113308A
-
|
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Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
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Metabolic Disease
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|
Taurolithocholic acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-P11615
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Bacterial
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Infection
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FuK is a WK2-analog antimicrobial peptide modified with fluorinated unnatural amino acids. FuK has an LD50 of 72.34 mg/kg in mice, shows no hemolytic activity, with high stability against trypsin, chymotrypsin, and saline environments. FuK exerts bactericidal effects by enhancing the permeability of bacterial outer membranes, inducing depolarization of cytoplasmic membranes, and disrupting membrane potential balance against bacterias such as Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and MRSA. FuK exhibits synergistic antimicrobial activity with polymyxin B (HY-149179), vancomycin (HY-B0671), and ciprofloxacin (HY-B0356), and also inhibits Ciprofloxacin-induced bacterial drug resistance. FuK has in vivo safety, effectively reduces bacterial load and inflammatory cell infiltration in a mouse MRSA model, and promotes collagen fiber formation in skin wounds .
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- HY-N6972
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Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Infection
Inflammation/Immunology
Cancer
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Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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-
- HY-169480
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Liposome
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Infection
Cancer
|
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Lipid C2 is an ionizable cationic lipid that has been used in the formation of lipid nanoparticles (LNP) for mRNA delivery in vivo. LNPs containing Lipid C2 and encapsulating an mRNA reporter selectively accumulate in the liver and spleen but not the heart, lungs, or kidneys in mice. LNP containing Lipid C2 and encapsulating mRNA encoding the Epstein-Barr virus (EBV) protein latent membrane protein 2 (LMP-2), in combination with an anti-programmed cell death protein 1 (PD-1) antibody, decrease tumor volume and reverse T cell exhaustion, as well as increase the percentage of CD3 +CD8 + central and CD3 +CD8 + effector memory T cells and decrease the percentage of CD3 + T cells expressing Pd-1, in the spleen in a CT26 murine EBV-infected colon cancer model .
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- HY-176428
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P11-2
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PROTACs
MNK
Apoptosis
Eukaryotic Initiation Factor (eIF)
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Cancer
|
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PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
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-
- HY-P992410
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PAI-1
TGF-beta/Smad
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Inflammation/Immunology
|
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MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
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- HY-125938
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Cycloartenol ferulate; Cycloartenol ferulic acid ester
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Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
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Inflammation/Immunology
Cancer
|
|
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
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- HY-174981
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PROTACs
FGFR
ATP Synthase
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Cancer
|
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LC-MF-4 is a selective FGFR3 PROTAC degrader with a DC50 of 30.89 nM in KMS-11 cells. LC-MF-4 inhibits the metabolic function of FGFR3-TACC3 fusion positive cancers with reduction of ATP synthesis and inhibition of mitochondrial biogenesis genes. LC-MF-4 has potent antitumor activity in the Ba/F3-FGFR3-TACC3 xenograft mice model. LC-MF-4 can be used for FGFR3-altered cancers like bladder cancer and urothelial carcinoma (UC) research . Pink: FGFR3 ligand (HY-175414); Blue: VHL ligase ligand (HY-125905); Black: linker (HY-Y1224)
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- HY-170621
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- HY-182033
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Bacterial
ClpP
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Infection
|
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ClpP agonist 1 is a Staphylococcus aureus ClpP (SaClpP) agonist with an EC50 of 1.44 μM, Kd values of 2.95 μM (isothermal titration calorimetry) and 18 μM (bio-layer interferometry), and a low drug resistance frequency. ClpP agonist 1 reduces bacterial load, shrinks infected area and improves histopathological outcomes in a mouse skin infection model. ClpP agonist 1 can be used for the research of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) skin infections .
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-
- HY-125847
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Ras
PI3K
Akt
Caspase
Apoptosis
Bcl-2 Family
NF-κB
MMP
|
Cancer
|
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Salvianolic acid F is a KRAS inhibitor, especially for KRAS G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of KRAS-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including KRAS G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer .
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-
- HY-183365
-
|
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SOS1
Ras
p38 MAPK
ERK
MEK
Apoptosis
|
Cancer
|
|
SL43 is an orally active and potent SOS1 inhibitor with a Kd of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model .
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- HY-D0186R
-
|
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Reference Standards
Endogenous Metabolite
Thymidylate Synthase
|
Infection
|
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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- HY-172371
-
|
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Hemoglobin
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
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Hypoxystat is an orally active hypoxia mimetic. HypoxyStat increases Hemoglobin’s oxygen affinity, limiting oxygen offloading to the tissues and inducing local tissue hypoxia. Hypoxystat reduces Iba1 + cells. HypoxyStat causes systemic hypoxia. Hypoxystat effectively rescues hyperglycemia in mouse models of type 1 and type 2 diabetes. HypoxyStat not only extends lifespan but also rescues key neuropathological and behavioral deficits in the premier mouse model of Leigh syndrome .
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- HY-183374
-
|
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Carbonic Anhydrase
Radionuclide-Drug Conjugates (RDCs)
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Cancer
|
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NYM074 is a carbonic anhydrase IX (CAIX) ligand. NYM074 binds specifically to human CAIX to enable targeted radionuclide delivery. NYM074 supports dual radiolabeling with 68Ga for positron emission tomography (PET) imaging and 177Lu for radionuclide applications. NYM074 can be used for the research of clear cell renal cell carcinoma .
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- HY-113308AS
-
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Isotope-Labeled Compounds
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
Metabolic Disease
|
|
Taurolithocholic acid-d4 (sodium) is the deuterium labeled Taurolithocholic acid (sodium salt). Taurolithocholic acid sodium is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-175521
-
|
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HIF/HIF Prolyl-Hydroxylase
IKK
NF-κB
Apoptosis
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC50 of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE) .
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- HY-113308AS2
-
|
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Isotope-Labeled Compounds
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
Metabolic Disease
|
|
Taurolithocholic acid-d4-1 (sodium) is the deuterium labeled Taurolithocholic acid. Taurolithocholic acid sodium is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-N6972R
-
|
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Autophagy
Reference Standards
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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- HY-113308S
-
|
|
Isotope-Labeled Compounds
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
Others
|
|
Taurolithocholic acid-d5 is deuterium labeled Taurolithocholic acid. Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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-
- HY-113308S1
-
|
|
Isotope-Labeled Compounds
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
Others
|
|
Taurolithocholic acid-d4 is deuterium labeled Taurolithocholic acid. Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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-
- HY-181088
-
|
|
Phosphodiesterase (PDE)
Interleukin Related
|
Metabolic Disease
|
|
PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury .
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-
- HY-113308AS1
-
|
|
Isotope-Labeled Compounds
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
Metabolic Disease
|
|
Taurolithocholic Acid-d5 (sodium) is the deuterium labeled Taurolithocholic acid sodium salt. Taurolithocholic Acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic Acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic Acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic Acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic Acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic Acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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-
- HY-114214
-
|
|
Drug Derivative
NF-κB
MMP
TNF Receptor
Interleukin Related
Cyclin G-associated Kinase (GAK)
CDK
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway . CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway . CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells . CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer .
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-
- HY-P991864
-
|
MDX-124
|
Formyl Peptide Receptor (FPR)
|
Cancer
|
|
Annexuzlimab is a humanised IgG1 monoclonal antibody which specifically binds to ANXA1 disrupting its interaction with formyl peptide receptors 1 and 2 (FPR1/2). Annexuzlimab arrests cell cycle progression with cancer cells accumulating in the G1 phase. Annexuzlimab targets secreted ANXA1, preventing FPR1/2 activation and reducing cancer progression. Annexuzlimab can be used for the research of triple negative breast cancer, pancreatic cancer and osteosarcoma .
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- HY-N0447
-
|
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TRP Channel
Bacterial
Apoptosis
Autophagy
STAT
PERK
EGFR
PI3K
Akt
mTOR
Caspase
MMP
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
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-
- HY-176798
-
|
|
Lactate Dehydrogenase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model .
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-
- HY-N0430
-
|
Coptisin
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
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-
- HY-120105
-
|
|
DNA/RNA Synthesis
Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
NSC666715 is a DNA polymerase β (Pol-β) inhibitor. NSC666715 directly and specifically interacts with Pol-β, interferes with its binding to damaged DNA, blocks its dRP lyase activity, and inhibits Pol-β-mediated SN- and LP-BER. NSC666715 induces AP site accumulation and S-phase cell cycle arrest, and triggers senescence and apoptosis (apoptosis) via the p53/p21 pathway in colorectal cancer cells. NSC666715 enhances TMZ (HY-17364)-induced DNA damage, senescence and apoptosis, and potentiates the cytotoxicity of TMZ. NSC666715 inhibits tumor growth in colon cancer xenograft models. NSC666715 can be used in research related to colorectal cancer .
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-
- HY-112817
-
|
8-Oxo-Deoxyguanosine triphosphate
|
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
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-
- HY-P1108
-
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CRFR
|
Neurological Disease
Inflammation/Immunology
|
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
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-
- HY-113308AR
-
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|
Reference Standards
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
Metabolic Disease
|
|
Taurolithocholic acid (sodium salt) (Standard) is the analytical standard of Taurolithocholic acid (sodium salt). This product is intended for research and analytical applications. Taurolithocholic acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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-
- HY-124084
-
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|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
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- HY-P991922
-
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Fc Receptor (FcR)
Complement System
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
AKIR001 is a high-affinity human IgG1 antibody targeting CD44v6. AKIR001 carries LALA-silencing mutations in its FcγR-binding domain to reduce FcγR and C1q interactions, minimizing tissue interactions and limiting CDC and ADCC risks. [ 177Lu] radiolabeled AKIR001, namely [ 177Lu]Lu-AKIR001, has anticancer activity against epidermoid carcinoma .
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- HY-186117
-
|
|
YAP
PROTACs
|
Cancer
|
|
KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer .
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-
- HY-181970
-
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|
Orphan Nuclear Receptor
Androgen Receptor
c-Myc
|
Cancer
|
|
XY25026 is an orally active LRH-1 inhibitor with an IC50 of 0.28 μM. XY25026 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells, suppresses the expression of AR target genes KLK2 and KLK3, and inhibits tumor growth in xenograft models. XY25026 is applicable to the research of castration-resistant prostate cancer .
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-
- HY-18326
-
|
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
BMS-869780 is an orally active non-acidic γ-secretase (γ-secretase) modulator. BMS-869780 regulates the activity of γ-secretase, thereby altering the production profile of β-amyloid proteins. When acting alone, it changes the relative levels of specific β-amyloid subtypes without inhibiting the total production of β-amyloid proteins. BMS-869780 exerts a synergistic effect with γ-secretase modulators of the acidic structural class to inhibit the total production of β-amyloid proteins in cell cultures .
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-
- HY-182456
-
|
|
KMO
|
Neurological Disease
|
|
CHDI-340246 is an orally active kynurenine monooxygenase (KMO) inhibitor. CHDI-340246 blocks KMO activity, alters the metabolic flux of the kynurenine pathway, inhibits the production of 3-hydroxykynurenine and quinolinic acid, elevates the levels of kynurenine and kynurenic acid, and restores electrophysiological abnormalities in transgenic mouse models of Huntington's disease. CHDI-340246 can be used in studies related to Huntington's disease .
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-
- HY-P10775A
-
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|
MMP
|
Cancer
|
|
BT1769 acetate is a conjugate and antitumor agent targeting MT1-MMP, with a Kd value of 3.35 nM against human targets. BT1769 acetate exhibits favorable pharmacokinetic properties. BT1769 acetate specifically binds to MT1-MMP via its bicyclic peptide component, delivering the cytotoxic agent MMAE (HY-15162) to antigen-expressing cells. It effectively inhibits tumor growth, induces complete responses, and significantly prolongs event-free survival in osteosarcoma patient-derived xenograft models. BT1769 acetate shows extremely low activity in Ewing sarcoma models and can be used in osteosarcoma-related research .
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-
- HY-182241
-
|
|
c-Myc
Early 2 Factor (E2F)
TNF Receptor
MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein . JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer .
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- HY-159768A
-
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|
Radionuclide-Drug Conjugates (RDCs)
FAP
|
Neurological Disease
Cancer
|
|
DOTAGA.Glu.(FAPi) 2 is a FAPI homodimer in which a central glutamic acid (Glu) linker connects FAPI and a chelator. Radiolabeled with gallium- 68, lutetium- 177 or terbium- 161, DOTAGA.Glu.(FAPi) 2 is applicable to FAP-positive cancer PET imaging studies. DOTAGA.Glu.(FAPi) 2 is suitable for research related to prostate adenocarcinoma and recurrent glioblastoma multiforme .
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-
- HY-W591838
-
|
PFPeS
|
Biochemical Assay Reagents
Phosphatase
|
Metabolic Disease
|
|
Perfluoropentanesulfonic acid (PFPeS) is a per- and polyfluoroalkyl substance. Perfluoropentanesulfonic acid increases alkaline phosphatase (ALKP). Perfluoropentanesulfonic acid induces systemic toxicity in mouse models and alters the expression of genes related to fatty acid metabolism, inflammation and skin integrity in the liver and skin .
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-
- HY-175318S
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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-
- HY-P11773
-
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|
Radionuclide-Drug Conjugates (RDCs)
Integrin
|
Others
|
|
3P-RGD2 is a dimeric cyclic RGD (Arg-Gly-Asp) peptide. When radiolabeled with 99mTc, 3P-RGD2 serves as a selective radiotracer for integrin αvβ3. When radiolabeled with 99mTc, 3P-RGD2 enables single-photon emission computed tomography imaging of integrin αvβ3 .
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-
- HY-181971
-
|
|
Orphan Nuclear Receptor
Androgen Receptor
c-Myc
|
Cancer
|
|
XY25028 is an orally active LRH-1 inhibitor with an IC50 of 0.30 μM. XY25028 inhibits the proliferation of androgen receptor (AR)-positive prostate cancer cells and suppresses the expression of AR target genes KLK2 and KLK3. XY25028 can be used in the research of castration-resistant prostate cancer .
|
-
- HY-181505
-
|
|
Epigenetic Reader Domain
c-Myc
Bcl-2 Family
PAK
Apoptosis
|
Cancer
|
|
BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC) .
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-
- HY-P1108A
-
|
|
CRFR
|
Neurological Disease
Inflammation/Immunology
|
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
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-
- HY-178061
-
|
|
ERK
RET
|
Cancer
|
|
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
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-
- HY-P10102
-
Kp7-6
2 Publications Verification
|
Apoptosis
PERK
NF-κB
Caspase
JNK
|
Inflammation/Immunology
Cancer
|
|
Kp7-6 is a Fas mimetic peptide and also a Fas/FasL antagonist. Kp7-6 specifically binds to Fas and FasL, disrupts receptor complexes, and blocks downstream apoptosis signaling pathways. Kp7-6 inhibits the phosphorylation of ERK1-2, induces the phosphorylation of IκBα, and activates NF-κB. Kp7-6 inhibits the activation of caspase-8, caspase-3 and JNK, and suppresses human amylin-induced β-cell apoptosis. Kp7-6 inhibits FasL-induced lymphoid cytotoxicity and apoptosis. Kp7-6 reduces local tumor FasL expression, increases CD8 +Fas + T cell infiltration, and decreases tumor volume in pancreatic neuroendocrine tumor models. Kp7-6 prevents concanavalin A-induced liver injury in mice. Kp7-6 is applicable to research related to type 2 diabetes, concanavalin A-induced hepatitis and pancreatic neuroendocrine tumors .
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- HY-177300
-
|
|
Toll-like Receptor (TLR)
HBV
IFNAR
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus .
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-
- HY-146272
-
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Vasopressin Receptor
|
Endocrinology
|
|
Vasopressin V2 receptor antagonist 1 is a vasopressin V2 receptor (V2R) antagonist with a Ki value of 3.8 nM. Vasopressin V2 receptor antagonist 1 inhibits renal cyst formation in embryonic renal cyst models and mouse models. Vasopressin V2 receptor antagonist 1 can be used in research related to autosomal dominant polycystic kidney disease .
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-
- HY-151093
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-
- HY-W071746R
-
|
Linoelaidic acid (Standard)
|
Reference Standards
Endogenous Metabolite
Parasite
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Linolelaidic acid (Standard) is the analytical standard of Linolelaidic acid. This product is intended for research and analytical applications. Linolelaidic acid (Linoelaidic acid) is an omega-6 trans fatty acid (TFA) that is an essential nutrient with oral activity. Linolelaidic acid can be added to enteral nutrition (oral), parenteral nutrition (intravenous), and infant formula. Linolelaidic acid has anti-inflammatory and anti-parasitic ((Parasite)) activities, and can induce Apoptosis. Linolelaidic acid is useful for research in infections[1][2][3].
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-
- HY-185492
-
-
- HY-P991550
-
|
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CD22
|
Cancer
|
|
RFB4 is an anti-CD22 monoclonal antibody. RFB4 can be fused with Pseudomonas aeruginosa exotoxin (PE38) via disulfide bonds to construct recombinant immunotoxins, such as RFB4 (dsFv)-PE38. RFB4 is applicable to the research of cancers including lymphoma .
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-
- HY-183576
-
|
|
HBV
|
Infection
Neurological Disease
|
|
HBsAg-IN-1 (Compound (6S,10S)-57) is an orally active, highly liver-selective inhibitor of HBsAg production, with an EC50 of 0.63 nM. HBsAg-IN-1 shows no neurite growth inhibitory activity. HBsAg-IN-1 can be used in studies related to hepatitis B virus (HBV) infection .
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-
- HY-172208
-
|
|
PROTACs
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
PROTAC cGAS degrader-1 is a potent and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 induces proteasome-mediated degradation of cGAS, inhibits the cGAS signaling pathway, and attenuates double-stranded DNA-induced activation of cGAS in human and mouse cells. PROTAC cGAS degrader-1 is applicable to research related to ulcerative colitis .
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-
- HY-182040
-
|
|
NF-κB
Heme Oxygenase (HO)
Interleukin Related
Reactive Oxygen Species (ROS)
NO Synthase
|
Inflammation/Immunology
|
|
Nrf2 activator-24 is a Nrf2 activator with anti-inflammatory and antioxidant activities. Nrf2 activator-24 promotes the nuclear translocation of Nrf2, thereby inducing the expression of downstream antioxidant and cytoprotective genes. Nrf2 activator-24 inhibits cytokine-driven inflammatory responses in keratinocytes. Nrf2 activator-24 attenuates inflammation, nitrosation and oxidative stress responses in macrophages. Nrf2 activator-24 alleviates local inflammation and atopic dermatitis-like symptoms in DNCB-induced mouse models. Nrf2 activator-24 can be used in research related to atopic dermatitis .
|
-
- HY-183557
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-6 is an orally active, blood-brain barrier-permeable O-GlcNAcase (OGA) inhibitor with an IC50 of 5.4 nM. O-GlcNAcase-IN-6 inhibits OGA activity, thereby increasing the level of O-GlcNAc glycosylation in brain tissues. O-GlcNAcase-IN-6 can be used for the research of Alzheimer's disease .
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-
- HY-113205
-
|
15-keto-PGE2
|
Endogenous Metabolite
Prostaglandin Receptor
STAT
PPAR
Fungal
Drug Metabolite
|
Cardiovascular Disease
Infection
Endocrinology
Cancer
|
|
15-keto-Prostaglandin E2 (15-keto-PGE2) is an endogenous PGE2 metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to the Cys259 residue of STAT3. 15-keto-Prostaglandin E2 binds to and stabilizes EP2 and EP4 receptors. 15-keto-Prostaglandin E2 inhibits the growth and progression of breast cancer cells. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth. 15-keto-Prostaglandin E2 disrupts glomerular vascularization during zebrafish development and reduces the surface area of the glomerular filtration barrier .
|
-
- HY-W071746
-
|
Linoelaidic acid
|
Endogenous Metabolite
Parasite
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Linolelaidic acid (Linoelaidic acid) is an omega-6 trans fatty acid (TFA) that is an essential nutrient with oral activity. Linolelaidic acid can be added to enteral nutrition (oral), parenteral nutrition (intravenous), and infant formula. Linolelaidic acid has anti-inflammatory and anti-parasitic ((Parasite)) activities, and can induce Apoptosis. Linolelaidic acid is useful for research in infections .
|
-
- HY-165360
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
JJ1 is a selective α-thrombin inhibitor with a Ki of 0.019 μM. JJ1 directly binds to the active site of α-thrombin to block its catalytic activity. JJ1 exhibits antithrombotic effects and prolongs activated partial thromboplastin time, prothrombin time, and tail bleeding time in mice. JJ1 can be used for the research of thrombotic diseases .
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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-
- HY-112817A
-
|
8-Oxo-Deoxyguanosine triphosphate trisodium
|
Apoptosis
|
Others
|
|
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP trisodium solution (100mM) acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP trisodium solution (100mM) causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP trisodium solution (100mM) in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP trisodium solution (100mM) is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
|
-
- HY-P4846
-
|
|
CXCR
Apoptosis
IFNAR
TNF Receptor
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and acts as a CXCR2 agonist . Ac-Pro-Gly-Pro-OH exerts bactericidal activity by generating hydrogen peroxide, inhibits pulmonary inflammation, and reduces immune cell apoptosis (apoptosis). Ac-Pro-Gly-Pro-OH promotes the production of IFN-γ and inhibits the production of TNF-α and IL-6 in leukocytes. Ac-Pro-Gly-Pro-OH increases the survival rate of mice in sepsis models, enhances the bactericidal activity of neutrophils, acts as a neutrophil chemoattractant, induces neutrophil polarization, and regulates inflammatory and repair processes. Ac-Pro-Gly-Pro-OH induces chronic inflammation and tissue remodeling through sustained action. Ac-Pro-Gly-Pro-OH is released via alkaline hydrolysis of corneal proteins in alkali-injured eyes, thereby driving the early infiltration of neutrophils into the cornea. Ac-Pro-Gly-Pro-OH is applicable to research related to sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcer .
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-
- HY-173629
-
|
|
Ras
Apoptosis
|
Cancer
|
|
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
|
-
- HY-D3141
-
|
|
|
Cancer
|
|
DR probe is a "dual-key-and-lock" fluorescent probe designed based on the Resorufin (HY-123533) scaffold (Ex/Em = 647 nm/663-738 nm). DR probe can be sequentially activated by hydrogen peroxide to form the intermediate SR, which acts as a tyrosinase substrate to trigger a fluorescence turn-on signal. DR probe can distinguish normal melanocytes from melanoma cells. DR probe supports cell imaging and can be applied to mouse melanoma models to achieve melanoma diagnosis with higher accuracy and lower false-positive rates. DR probe is applicable to relevant research on melanoma .
|
-
- HY-150520
-
|
|
Antibiotic
Phospholipase
|
Infection
Cancer
|
|
Neomycin, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin is a known phospholipase C (PLC) inhibitor. Neomycin potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin can be used for the research of cancer .
|
-
- HY-172699
-
|
|
Liposome
LDLR
|
Cancer
|
|
DSPE-PEG2000-ANG is a conjugate of DSPE-PEG2000-MAL and Angiopep-2. Angiopep-2 is a peptide ligand that targets LRP-1. DSPE-PEG2000-ANG is used to synthesize gadolinium-boron bifunctionalized lipid nanoparticles BPA-F&DOTA-Gd@LIPO-ANG with blood-brain barrier and glioma targeting properties .
|
-
- HY-181849
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .
|
-
- HY-B0470
-
|
|
Environmental Pollutants
Antibiotic
Phospholipase
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin sulfate inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin sulfate depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin sulfate can be used for the research of cancer .
|
-
- HY-181517
-
|
|
Bacterial
|
Infection
Cancer
|
|
Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study .
|
-
- HY-182030
-
|
|
RSV
|
Infection
|
|
RSV fusion protein IN-1 is an orally active RSV pre-fusion F protein inhibitor with an IC50 of 0.10 nM against RSV. RSV fusion protein IN-1 forms stable hydrogen bonds and π-π stacking interactions with pre-fusion F protein to block viral fusion and entry. RSV fusion protein IN-1 suppresses RSV F protein expression in epithelial cells. RSV fusion protein IN-1 reduces viral burden in the lungs of RSV-infected murine models.RSV fusion protein IN-1 can be used for the research of respiratory syncytial virus (RSV) infection .
|
-
- HY-185561
-
|
RC88
|
Mesothelin
|
Cancer
|
|
Misitatug blivedotin (RC88) is an antibody-drug conjugate (ADC) targeting mesothelin (MSLN). Misitatug blivedotin binds to mesothelin and exhibits dose‐dependent antitumor activity. Misitatug blivedotin can be used for the research of ovarian cancer, non-squamous non-small-cell lung carcinoma, cervical cancer .
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-
- HY-183296
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
Caspase
|
Inflammation/Immunology
|
|
NLRP3-IN-91 is a potent NLRP3 inflammasome inhibitor with a Kd of 558.4 nM. NLRP3-IN-91 directly targets the NLRP3 NACHT domain, blocks inflammasome assembly and activation, and exerts anti-inflammatory effects. NLRP3-IN-91 increases survival time in a murine model of LPS (HY-D1056)-induced sepsis. NLRP3-IN-91 can be used for the research of sepsis .
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-
- HY-183593
-
|
|
Phosphatase
Akt
Interleukin Related
|
Neurological Disease
|
|
SHIP1-IN-1 is an orally active, blood-brain barrier-permeable SHIP1 ligand. SHIP1-IN-1 exhibits IC50 values of 384 μM and 177 μM against human SHIP1, and an IC50 value of 379 μM against murine SHIP1. SHIP1-IN-1 alters the binding state of SHIP1 to phosphatidylinositol membranes, and regulates phosphoinositide pools and phosphorylated AKT levels. SHIP1-IN-1 enhances the uptake of myelin/membrane fragments and amyloid proteins by microglia, alters gene expression and reduces IL-1β levels. SHIP1-IN-1 can be used in studies related to Alzheimer's disease .
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-
- HY-183333
-
|
|
Fungal
|
Infection
|
|
CHNQD-02204 is a potent and selective antifungal agent with in vitro activity against Candida albicans, with a MIC of 0.025 μg/mL. CHNQD-02204 inhibits ergosterol biosynthesis, disrupts the membrane integrity and biofilm formation of Candida albicans, and suppresses the morphological transition of Candida albicans from yeast to hyphal form. CHNQD-02204 can be used in studies related to candidal infections .
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-
- HY-P4610
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
H-Trp-Tyr-OH is an orally active tryptophan-tyrosine dipeptide with blood-brain barrier permeability. H-Trp-Tyr-OH exerts physiological regulatory effects by stimulating enteroendocrine cells to secrete glucagon-like peptide GLP-1. In mouse models of tauopathies, H-Trp-Tyr-OH inhibits tau phosphorylation, reduces the level of neurofibrillary tangles, increases dopamine turnover, upregulates synapsin expression, and elevates cecal short-chain fatty acid levels, thereby improving behavioral deficits and extending lifespan. H-Trp-Tyr-OH can be used in research related to impaired glucose tolerance and tauopathies .
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-
- HY-182034
-
|
|
Toll-like Receptor (TLR)
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
GAP214 is a monosaccharide lipid A analogue and TLR4/MD-2 complex modulator.GAP214 binds to the TLR4/MD-2 complex via hydrophobic interactions, salt bridges, and hydrogen bonds, induces dimerization of the complex to initiate intracellular signaling cascades.GAP214 functions as an immunostimulant and vaccine adjuvant, enhances antigen-specific IgG antibody production in a mouse model .
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-
- HY-183370
-
|
|
JAK
STAT
Interleukin Related
|
Inflammation/Immunology
|
|
JAK2/STAT3-IN-2 is an orally active JAK2/STAT3 inhibitor. JAK2/STAT3-IN-2 inhibits the phosphorylation of tyrosine residues in JAK2 and STAT3, blocks downstream signal transduction, disrupts the dimerization and nuclear translocation of STAT3, and suppresses pro-inflammatory transcriptional activity. JAK2/STAT3-IN-2 inhibits the expression of IL-17A and IL-17F, reduces immune cell infiltration, and inhibits the production of NO simultaneously. JAK2/STAT3-IN-2 exerts a protective effect in a mouse model of ulcerative colitis induced by DSS (HY-116282C). JAK2/STAT3-IN-2 can be used for the research of ulcerative colitis .
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-
- HY-155033
-
|
|
Stearoyl-CoA Desaturase (SCD)
DNA/RNA Synthesis
Apoptosis
Autophagy
mTOR
Influenza Virus
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
SSI-4 is an orally active stearoyl-CoA desaturase (SCD1) inhibitor with an EC50 of 1.9 nM against mouse SCD1. SSI-4 blocks the conversion of saturated fatty acids to monounsaturated fatty acids, reducing the production of oleic acid and palmitoleic acid. SSI-4 induces lipid peroxidation, endoplasmic reticulum stress, DNA damage and activates apoptotic mechanisms. SSI-4 inhibits mTORC1 activity, suppresses B cell proliferation and antibody production, and induces autophagy. SSI-4 is applicable to research on cancers such as acute myeloid leukemia and renal cell carcinoma, as well as influenza infections .
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-
- HY-180372
-
-
- HY-P991228
-
|
|
Galectin
|
Cancer
|
|
LYT-200 is a humanized monoclonal antibody against galectin-9 (Galectin-9). LYT-200 binds to galectin-9 expressed on the surface of hematologic malignant cells, inhibits pro-leukemic functions and induces cell death. LYT-200 can be used in research related to hematologic malignancies .
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-
- HY-P991004
-
|
LB-101
|
CD47
PD-1/PD-L1
|
Cancer
|
|
Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
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-
- HY-176761
-
|
|
Apoptosis
Autophagy
Caspase
mTOR
|
Cancer
|
|
NSC647889 is an apoptosis and autophagy inducer. NSC647889 induces apoptosis, inhibits mTOR pathway and abrogates DNA synthesis. NSC647889 triggers LC3-positive vesicle formation, modulates AKT and 4EBP1 phosphorylation and shows heightened caspase-3 activation in multicellular spheroids. NSC647889 can be used for the research of solid cancer tumour, head-neck carcinoma, and colorectal cancer .
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-
- HY-143657
-
|
|
Myosin
Ferlin Family
MMP
|
Cancer
|
|
Myoferlin inhibitor 1 is a compound that exhibits reversible, concentration-dependent binding to the myoferlin MYOF-C2D protein, with a KD of 0.094 μM. Myoferlin inhibitor 1 shows potent anti-invasion and anti-migration activities against different pancreatic cancer cells. Myoferlin inhibitor 1 inhibits pancreatic cancer metastasis through reversing mesenchymal transition (EMT), inhibiting the secretions of MMP1 and MMP2 and blocking the receptor tyrosine kinases. Myoferlin inhibitor 1 displays effective antimetastatic activities in pancreatic cancer in vitro and in vivo. Myoferlin inhibitor 1 can be used in research on preventing pancreatic cancer metastasis .
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-
- HY-P11303
-
|
|
CD74
MHC
|
Neurological Disease
Cancer
|
|
PADRE peptide is a pan-HLA-DR binding epitope and immunostimulant. PADRE peptide binds to the peptide-binding groove of MHC class II molecules for presentation to CD4 + T cells, thereby effectively stimulating specific immune responses. PADRE peptide not only enhances anti-tumor immune responses, inhibits tumor growth and prolongs survival; it also significantly increases the frequency of E7-specific CD8 + T cells and improves therapeutic efficacy against TC-1 tumors when used in combination with E7 peptide-based vaccines and poly (I:C). The intensity of the immune response induced by PADRE peptide is lower than that of the Ii-PADRE DNA vaccine, and it fails to enhance the immune effect of CRT-E7 DNA. PADRE peptide is widely applicable to research on related tumors such as melanoma, glioblastoma and cervical cancer .
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-
- HY-182378
-
|
|
|
Cancer
|
|
Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC50 categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer .
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-
- HY-D3168
-
|
|
Fluorescent Dye
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
PCL-2 is a reactive oxygen species-responsive fluorescent probe that shows almost no response to biologically relevant reactive oxygen species other than hydrogen peroxide. PCL-2 reacts with hydrogen peroxide to release 6-hydroxy-2-cyanobenzothiazole. PCL-2 can be used for chemoselective imaging of hydrogen peroxide in in vitro models and acute inflammation mouse models. PCL-2 is applicable to studies related to acute inflammation .
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-
- HY-P990953
-
|
Gen1047
|
CD3
|
Cancer
|
|
Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
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-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
Bacterial
Apoptosis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
PARP
MMP
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
NF-κB
mTOR
Lactate Dehydrogenase
CDK
Glutathione Peroxidase
SOD
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
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-
- HY-168894
-
|
|
Ferroptosis
JAK
STAT
p38 MAPK
AMPK
GSK-3
Apoptosis
HSP
TNF Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
CT-1 is a secreted protein belonging to the IL-6 cytokine family. Overexpression of CT-1 enhances cell proliferation, migration and angiogenesis via the ADMA/DDAH pathway. CT-1 inhibits the growth of triple-negative breast cancer cells by simultaneously inducing Ferroptosis in N2-type tumor-associated neutrophils and cancer cells. CT-1 activates the Jak/STAT-3, p42/p44 MAPK and AMPK pathways, and inhibits GSK-3β activity through phosphorylation to induce cardiomyocyte hypertrophy. CT-1 enhances the viability of cardiomyocytes and neurons, reduces cell Apoptosis, induces the expression of heat shock proteins (HSP) and BNP, and inhibits TNF levels. CT-1 exerts anti-tumor activity in mouse models of triple-negative breast cancer. CT-1 improves cognitive impairment in mice. CT-1 is applicable to the research of ischemic heart disease, triple-negative breast cancer, myocardial hypertrophy, Parkinson's disease, hypertensive heart disease, myocardial infarction, acute Chagas cardiomyopathy, high-fat diet-induced cognitive impairment and diabetes-related cognitive impairment .
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- HY-N0171R
-
|
β-Sitosterol (Standard); 22,23-Dihydrostigmasterol (Standard))
|
Reference Standards
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (Standard) is the analytical standard of Beta-Sitosterol. This product is intended for research and analytical applications. Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
|
-
- HY-N0171
-
|
|
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
- HY-N0120
-
|
(E/Z)-Piceid
|
Drug Isomer
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
(E/Z)-Polydatin ((E/Z)-Piceid) is a mixture of the E/Z configurations of Polydatin (HY-N0120A). Polydatin can be isolated from Polygonum cuspidatum, grapes, peanuts, red wine, hop pellets, cocoa-containing products and chocolate products. Polydatin exhibits multiple biological properties, such as anti-platelet aggregation, anti-low-density lipoprotein oxidation, cardioprotective activity, anti-inflammatory and immunomodulatory functions. Polydatin shows favorable cytotoxic effects against various tumor cell lines, including cervical cancer cells, liver cancer cells, and nasopharyngeal carcinoma cells .
|
-
- HY-133151
-
|
|
CXCR
|
Cancer
|
|
CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma .
|
-
- HY-P990914
-
|
GS-1811; JTX-1811
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a KD of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstream CCR8 signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology .
|
-
- HY-P10427
-
|
|
CXCR
Dengue Virus
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
|
-
- HY-159102
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
PVP-037.2 is a TLR7/8 agonist. PVP-037.2 can serve as an adjuvant to enhance vaccine-induced TH1 type immune responses, increasing the production of antigen-specific antibodies IgG1 and IgG2c .
|
-
- HY-10823
-
|
GW1843; 1843U89; OSI-7904
|
Thymidylate Synthase
DNA/RNA Synthesis
|
Cancer
|
|
OSI-7904L (GW1843; 1843U89; OSI-7904) is a thymidylate synthase (TS) inhibitor with a Ki of 90 pM. OSI-7904L blocks de novo synthesis of thymidine nucleotides, DNA synthesis and induces cell death. OSI-7904L inhibits the growth of human cells, induces tumor regression, and achieves durable antitumor effects in mouse xenograft models. OSI-7904L can be used in research related to colon adenocarcinoma .
|
-
- HY-N19281
-
|
|
Drug Derivative
|
Neurological Disease
|
|
Puberulin is a coumarin compound and an orally effective analgesic. Puberulin is present in Choisya ternata var. Sundance. Puberulin exerts analgesic activity against chemical and heat-induced pain agents in mouse models, and this activity does not involve opioid receptors or muscarinic receptors. Puberulin can be used in the research of neuropathic pain .
|
-
- HY-123795
-
|
|
Ras
Akt
ERK
VEGFR
|
Cancer
|
|
NY0123 is a EPAC1 inhibitor. NY0123 significantly inhibits the expression of EPAC1, phosphorylated AKT, phosphorylated ERK1/2 and phosphorylated VEGFR2. NY0123 inhibits angiogenesis and tumor growth of triple-negative breast cancer. NY0123 is applicable to relevant research on triple-negative breast cancer .
|
-
- HY-181976
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Others
|
|
dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 specifically recruits the first bromodomain of BRD4 to the E3 ubiquitin ligase complex (SCF FBXO3), thereby triggering the ubiquitination and degradation of BRD4 .
|
-
- HY-162588
-
|
|
NOD-like Receptor (NLR)
ATTECs
Autophagy
|
Inflammation/Immunology
|
|
MC-ND-18 is an ATTEC degrader that degrades NLRP3 via the Autophagy pathway, with a DC50 of 125.5 nM in THP-1 cells. MC-ND-18 exhibits anti-inflammatory activity in a DSS-induced mouse model of colitis. MC-ND-18 can be used for research on inflammatory bowel disease. MC-ND-18 consists of an NLRP3 inhibitor (HY-156121), a linker (HY-W018745), and an LC3 ligand .
|
-
- HY-183308
-
|
|
Fungal
|
Infection
|
|
Antifungal agent-161 (Compound 7) is an Antifungal agent. Antifungal agent-161 potently inhibits Candida albicans ATCC 36082 (with a MIC of 1.32 μM) and Candida glabrata ATCC 2001 (with a MIC of 1.66 μM). Antifungal agent-161 reduces fungal loads in infected mice and eliminates Candida albicans and Candida glabrata infections. Antifungal agent-161 can be used for the research of candidiasis .
|
-
- HY-181080
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
TOP1/TDP1-IN-1 is a DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with a TDP1 IC50 of 17.8 μM. TOP1/TDP1-IN-1directly suppresses TOP1 catalytic activity without forming a DNA-TOP1 ternary complex, inhibits TDP1-mediated repair of TOP1-induced DNA damage, and exhibits low acute toxicity. TOP1/TDP1-IN-1 disrupts DNA repair pathways, induces apoptosis, suppresses clonogenic growth, and elicits antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be used for the research of non-small cell lung cancer, cervical cancer, colon cancer .
|
-
- HY-182685
-
|
|
Acetyl-CoA synthetase
Parasite
|
Infection
|
|
MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC50 of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .
|
-
- HY-P992151
-
|
LT1002
|
LPL Receptor
Interleukin Related
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Sphingomab (LT1002) is a mouse-derived IgG1 κ monoclonal antibody and also an inhibitor targeting S1P, with high affinity for S1P and a Kd value of 0.03 ± 0.002 nM. Sphingomab blocks S1P-mediated IL-8 release in ovarian cancer cells. Sphingomab exhibits anti-angiogenic activity in a mouse model of choroidal neovascularization. Sphingomab reduces peripheral blood lymphocyte counts. Sphingomab can be used in the research of ovarian cancer and age-related macular degeneration .
|
-
- HY-186103
-
|
|
CD1
IFNAR
Interleukin Related
Bacterial
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Glycolipid C34, α-GalCer (HY-102022) analog, is a CD1d-binding glycolipid antinfection agent. Glycolipid C34 mediates invariant natural killer T cell activation and increases the secretion of IFN-γ and IL-4. Glycolipid C34 promotes clearance of bacterial infections in murine models and enhances protective immunity against viral infections. Glycolipid C34 can be used for the research of bacterial infection, viral infection .
|
-
- HY-175610
-
|
|
PROTACs
FLT3
JAK
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
|
-
- HY-B2167R
-
|
DHA (Standard); Cervonic acid (Standard)
|
Reference Standards
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
|
-
- HY-N0493
-
|
|
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
|
-
- HY-N0493R
-
|
|
Reference Standards
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
Inflammation/Immunology
|
|
Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
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- HY-122557
-
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Neurological Disease
|
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AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT1A and 5-HT1B receptors, with nanomolar binding affinity for human and monkey receptors (human 5-HT1A: 0.16 nM, monkey 5-HT1A: 0.13 nM, human 5-HT1B: 2.3 nM, monkey 5-HT1B: 2.4 nM). AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease .
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- HY-118970
-
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VD/VDR
TGF-β Receptor
Interleukin Related
|
Cancer
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LG190155 is a nonsteroidal vitamin D receptor (VDR) agonist. LG190155 activates VDR in mesenchymal stem cells, thereby upregulating the BMP6-IL6 autocrine axis. Pretreatment of mesenchymal stem cells with LG190155 significantly enhances their ability to induce differentiation of acute myeloid leukemia cells, without inducing hypercalcemia. LG190155 is applicable to research related to acute myeloid leukemia (AML) .
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- HY-14668
-
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AEGR-733 mesylate; BMS-201038 mesylate
|
Microsomal Triglyceride Transfer Protein (MTP)
mTOR
LDLR
Autophagy
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein (MTP) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein (VLDL). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK-independent autophagic cell death and suppressing cancer cell growth and apoptosis. Lomitapide mesylate also enhances tumor infiltration of CD8 + T cells. In addition, Lomitapide mesylate inhibits HDAC, improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer, breast cancer, melanoma, ischemic stroke, and familial hypercholesterolemia .
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- HY-P991883
-
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Licartin; Metuximab; Mehuzumab
|
Apoptosis
CDK
Caspase
Bcl-2 Family
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Cancer
|
|
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
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- HY-P991902
-
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CD20
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Cancer
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NAV006 is an anti-CD20 antibody variant of Rituximab (HY-P9913) with a Kd of 30.5 nM to CD20. NAV006 exhibits reduced interaction with CA125 and demonstrates enhanced antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) activity. NAV006 displays antitumor activity against lymphoma and can be used in research on non-Hodgkin lymphoma .
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- HY-P1907
-
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HPV
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Cancer
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Human Papillomavirus (HPV) E7 protein (49-57) is a cytotoxic T lymphocyte (CTL) epitope peptide derived from HPV16 E7 protein (sequence: RAHYNIVTF). Human Papillomavirus (HPV) E7 protein (49-57) induces E749-57-specific CTL responses. Human Papillomavirus (HPV) E7 protein (49-57) can be used for the research of cervical cancer .
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- HY-124627
-
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Estrogen Receptor/ERR
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Cancer
|
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THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor ERα degrader (SERD) (IC50=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer .
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-
- HY-W002942
-
|
1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline
|
Ferroptosis
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
|
Ferroptosis-IN-21 is a ferroptosis inhibitor that protects against renal I/R injury by suppressing ferroptosis and directly scavenging peroxyl radicals. Ferroptosis-IN-21 displays broad-spectrum anti-ferroptotic efficacy across multiple inducers in renal tubular epithelial cells, with nanomolar potency and robust suppression of lipid Reactive Oxygen Species (ROS). Ferroptosis-IN-21 significantly ameliorates renal I/R injury in mice, reducing histological damage, functional impairment, and inflammatory cytokine expression, while decreasing lipid peroxidation biomarkers such as 4-hydroxynonenal. Ferroptosis-IN-12 can be used for research in the field of ferroptosis-targeted drug development .
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- HY-123606
-
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Protein Arginine Deiminase
MHC
|
Cardiovascular Disease
Inflammation/Immunology
|
|
GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8 + T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions .
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-
- HY-175340
-
|
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Potassium Channel
TSPO
|
Neurological Disease
|
|
Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .
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- HY-181991
-
|
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Virus Protease
Flavivirus
|
Infection
|
|
IRBM-Z-2 is a non-competitive, orally active Zika virus (ZIKV) NS2B-NS3 protease inhibitor, with IC50 values of 0.04 μM and 3.1 μM against the wild-type and I156T mutant strains, respectively. IRBM-Z-2 exhibits broad-spectrum anti-flavivirus potential, with IC50 values of 2.1 μM and 0.09 μM against the NS2B-NS3 proteases of dengue virus 2 (DENV2) and West Nile virus (WNV), respectively. IRBM-Z-1 inhibits ZIKV replication and alleviates virus-induced cytopathic effects. IRBM-Z-1 can be used in studies related to ZIKV infection .
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-
- HY-183784
-
|
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P2X Receptor
FAK
MMP
|
Cancer
|
|
P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research .
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-
- HY-12929
-
|
SU093
|
Pim
Apoptosis
|
Cancer
|
|
NSC756093 (SU093) is a GBP1:PIM1 interaction inhibitor. NSC756093 binds to GBP1-PIM1 with a Kd of 38 nM. NSC756093 suppresses proliferation, reduces migration, induces G1 phase cell-cycle arrest, and increases apoptotic cell death in ovarian cancer cells. NSC756093 reduces cellular proteasomal activity, induces accumulation of ubiquitinated proteins, and restrains tumor progression and lung metastasis in murine ovarian cancer xenograft models. NSC756093 increases sensitivity of prostate cancer cells to Docetaxel (HY-B0011) and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel (HY-B0015). NSC756093 can be used for the research of prostate cancer and ovarian cancer .
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-
- HY-W011592
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
N-Phthaloyl-L-glutamic acid is an orally active anti-inflammatory agent. N-Phthaloyl-L-glutamic acid inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced nitric oxide production in murine spleen cells. N-Phthaloyl-L-glutamic acid does not exhibit significant cytotoxicity in vitro against tumor cells and BALB/c mice spleen cell culture. N-Phthaloyl-L-glutamic acid can be used for the research of inflammation .
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-
- HY-186072
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
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-
- HY-155887
-
|
DSPE-PEG-NH2, MW 3400 ammonium
|
Liposome
|
Cancer
|
|
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
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-
- HY-141878
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
di-Ellipticine-RIBOTAC is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
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-
- HY-141878A
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
di-Ellipticine-RIBOTAC TFA is a RNase recruiting chimera (RIBOTAC) degrader, capable of specifically binding and degrading expanded G4C2 RNA repeat (r(G4C2) exp). di-Ellipticine-RIBOTAC TFA selectively binds the three-dimensional (3D) structure formed by r(G4C2) exp and that recruits an endogenous ribonuclease (RNase) to cleave r(G4C2) exp. di-Ellipticine-RIBOTAC TFA selectively degrades the mutant chromosome 9 open reading frame 72 (C9orf72) allele and reduces quantities of toxic dipeptide repeat proteins (DPRs) translated from r(G4C2) exp. di-Ellipticine-RIBOTAC TFA significantly improves the pathological phenotype of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) in cells and mouse models. di-Ellipticine-RIBOTAC TFA can be used for the study of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD) .
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-
- HY-P991924
-
-
- HY-186073
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury .
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-
- HY-P991896
-
|
AT14-012
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
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-
- HY-P991935
-
|
|
Apoptosis
|
Cancer
|
|
ANT1034 is humanized anti-CD52 antibody. ANT1034 directs antibody dependent and complement dependent cell cytotoxicity, induces Apoptosis when cross-linked or in the presence of a cross-linking antibody. ANT1034 leads to increased survival in a SCID CD52 tumour xenograft model. ANT1034 can be used for the research of B cell malignancies .
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-
- HY-180419
-
|
|
ERK
Apoptosis
c-Myc
|
Inflammation/Immunology
Cancer
|
|
SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup .
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-
- HY-181010
-
|
|
HDAC
Parasite
|
Infection
|
|
HDAC1-IN-12 is a Plasmodium falciparum HDAC1 (PfHDAC1) inhibitor with an IC50 of 4.1 nM against Pf3D7. HDAC1-IN-12 inhibits PfHDAC1, upregulates histone H3 acetylation in P. falciparum parasites, downregulates malaria invasion-related gene expression, and exhibits favorable safety profiles, improved physicochemical properties, and potent in vivo antimalarial activity. HDAC1-IN-12 can be used for the research of malaria .
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-
- HY-12761
-
|
|
Cannabinoid Receptor
|
Cardiovascular Disease
Others
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H2O2). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc .
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-
-
-
HY-L217
-
|
|
330 compounds
|
|
Metabolic abnormalities lead to dysfunction of metabolic pathways and the accumulation or lack of metabolites, which are recognized hallmarks of the disease. The metabolite signature is closely related to the disease phenotype and is very useful for predicting the diagnosis and prognosis of the disease as well as monitoring treatment. Metabolites can be used as disease markers for diagnostic therapy. As the classic model of disease experiment in vivo, mice metabolites also play a role in disease diagnosis and mechanism research.
MCE provides 330 mouse metabolites that can be used in disease research.
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| Cat. No. |
Product Name |
Type |
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
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-
- HY-107202GL
-
|
Poly(I:C) (GMP Like)
|
Fluorescent Dye
|
|
Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
|
-
- HY-16561G
-
|
trans-Resveratrol; SRT501
|
Fluorescent Dye
|
|
Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-D2279
-
|
|
Fluorescent Dye
|
|
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively .
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-
- HY-D3186
-
|
|
Fluorescent Dye
|
|
HMRef-βGal is a fluorescent probe and a substrate responsive to β-galactosidase (β-galactosidase) (Ex/Em=498 nm/505-600 nm). After being cleaved by β-galactosidase, HMRef-βGal triggers significant fluorescence enhancement via intramolecular spirocyclic function regulation. HMRef-βGal generates bright fluorescence in cancer cells with elevated β-galactosidase activity, enabling visualization of tiny peritoneal metastases in mouse models. HMRef-βGal exhibits low in vitro cytotoxicity and low acute in vivo toxicity in mice. HMRef-βGal can be used for preclinical fluorescence-guided diagnosis and cytoreductive surgery of peritoneal metastases, including compatibility with real-time naked-eye detection and endoscopic imaging, as well as for studies related to peritoneal metastases of ovarian cancer .
|
-
- HY-D3220
-
|
|
Fluorescent Dye
|
|
PTO-41 is a blood-brain barrier-permeable near-infrared fluorescent probe that targets β-amyloid oligomers (Aβ Oligomers, AβOs) with a Kd of 349 nM. PTO-41 exhibits low cytotoxicity, high sensitivity to β-amyloid oligomers in in vitro phantom imaging, and can be rapidly cleared from the brain. PTO-41 is applicable to the research of Alzheimer's disease (Ex/Em = 538 nM/680 nM) .
|
-
- HY-D3141
-
|
|
Fluorescent Dye
|
|
DR probe is a "dual-key-and-lock" fluorescent probe designed based on the Resorufin (HY-123533) scaffold (Ex/Em = 647 nm/663-738 nm). DR probe can be sequentially activated by hydrogen peroxide to form the intermediate SR, which acts as a tyrosinase substrate to trigger a fluorescence turn-on signal. DR probe can distinguish normal melanocytes from melanoma cells. DR probe supports cell imaging and can be applied to mouse melanoma models to achieve melanoma diagnosis with higher accuracy and lower false-positive rates. DR probe is applicable to relevant research on melanoma .
|
-
- HY-D3168
-
|
|
Fluorescent Dye
|
|
PCL-2 is a reactive oxygen species-responsive fluorescent probe that shows almost no response to biologically relevant reactive oxygen species other than hydrogen peroxide. PCL-2 reacts with hydrogen peroxide to release 6-hydroxy-2-cyanobenzothiazole. PCL-2 can be used for chemoselective imaging of hydrogen peroxide in in vitro models and acute inflammation mouse models. PCL-2 is applicable to studies related to acute inflammation .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W088065
-
|
|
Biochemical Assay Reagents
|
Sodium formate acts as a key promoter for heterogeneous nucleation of ZIF crystals and thin film synthesis. It is also recognized as a GRAS substance by the FDA, and serves as a cosmetic preservative and food additive. Sodium formate has low acute oral toxicity (acute oral LD50=7410 mg/kg and acute intravenous LD50=807 mg/kg in mice), with no heritable or carcinogenic effects, but exhibits embryonic developmental toxicity and teratogenicity at high concentrations. Sodium formate may cause moderate irritation to rabbit eyes, is relatively safe to the skin, and does not induce tumor formation in rats in vivo. Sodium formate is rapidly absorbed and oxidized to carbon dioxide in vivo, and forms DNA adducts in specific metabolic deficiency models or upon high-dose exposure .
|
-
- HY-107202GL
-
|
Poly(I:C) (GMP Like)
|
Biochemical Assay Reagents
|
|
Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
|
-
- HY-172699
-
|
|
Biochemical Assay Reagents
|
|
DSPE-PEG2000-ANG is a conjugate of DSPE-PEG2000-MAL and Angiopep-2. Angiopep-2 is a peptide ligand that targets LRP-1. DSPE-PEG2000-ANG is used to synthesize gadolinium-boron bifunctionalized lipid nanoparticles BPA-F&DOTA-Gd@LIPO-ANG with blood-brain barrier and glioma targeting properties .
|
-
- HY-155887
-
|
DSPE-PEG-NH2, MW 3400 ammonium
|
Biochemical Assay Reagents
|
|
DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
|
-
- HY-16561G
-
|
trans-Resveratrol; SRT501
|
Biochemical Assay Reagents
|
|
Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5912
-
|
|
iGluR
Calcium Channel
|
Neurological Disease
|
|
GluN1 (356-385) is a polypeptide targeting NMDAR GluN1. GluN1 (356-385) induces the production of autoantibodies, which reduce the density of cell surface NMDAR clusters, impair long-term potentiation, and decrease NMDAR-mediated Ca 2+ influx. As an immunogen, GluN1 (356-385) induces symptoms similar to anti-NMDAR encephalitis, including memory loss, in mice. GluN1 (356-385) can be used to establish a mouse model that mimics the pathogenesis of anti-NMDAR encephalitis. GluN1 (356-385) is applicable to research related to anti-NMDAR encephalitis .
|
-
- HY-P4094
-
CTP
2 Publications Verification
Cardiac targeting peptide
|
Peptides
|
Cardiovascular Disease
|
|
CTP (cardiac targeting peptide) can transduce cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be reversibly linked (e.g. via enolases, thiol groups) to cargo (e.g. miRNAs) for delivery specifically to cardiomyocytes over all other organs .
|
-
- HY-P1408
-
|
|
Integrin
VEGFR
|
Cancer
|
|
Obtustatin is a non-RGD disintegrin consisting of 41 residues. Obtustatin inhibits the adhesion of α1β1 integrin to type IV Collagen (HY-NP003), blocks α1β1 integrin signaling in endothelial cells, and suppresses FGF2-induced angiogenesis. Obtustatin inhibits tumor progression in mouse models and upregulates VEGF expression in sarcoma-bearing mice. Obtustatin can be used in research related to Lewis lung carcinoma and S-180 sarcoma .
|
-
- HY-P5128
-
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Satoreotide tetraxetan
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
|
DOTA-JR11 is a somatostatin receptor 2 (SSTR2)antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research . DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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-
- HY-P10102
-
Kp7-6
2 Publications Verification
|
Apoptosis
PERK
NF-κB
Caspase
JNK
|
Inflammation/Immunology
Cancer
|
|
Kp7-6 is a Fas mimetic peptide and also a Fas/FasL antagonist. Kp7-6 specifically binds to Fas and FasL, disrupts receptor complexes, and blocks downstream apoptosis signaling pathways. Kp7-6 inhibits the phosphorylation of ERK1-2, induces the phosphorylation of IκBα, and activates NF-κB. Kp7-6 inhibits the activation of caspase-8, caspase-3 and JNK, and suppresses human amylin-induced β-cell apoptosis. Kp7-6 inhibits FasL-induced lymphoid cytotoxicity and apoptosis. Kp7-6 reduces local tumor FasL expression, increases CD8 +Fas + T cell infiltration, and decreases tumor volume in pancreatic neuroendocrine tumor models. Kp7-6 prevents concanavalin A-induced liver injury in mice. Kp7-6 is applicable to research related to type 2 diabetes, concanavalin A-induced hepatitis and pancreatic neuroendocrine tumors .
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-
- HY-P11287A
-
|
|
Interleukin Related
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
DOTA-Pep-1L TFA is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L TFA specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L TFA yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L TFA can be used for PET imaging, tumor targeting and glioma research .
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-
- HY-P1108
-
|
|
CRFR
|
Neurological Disease
Inflammation/Immunology
|
Astressin 2B is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
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- HY-P1108A
-
|
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CRFR
|
Neurological Disease
Inflammation/Immunology
|
Astressin 2B TFA is a blood-brain barrier-impermeable, highly selective CRFR2 antagonist (rCRFR2, IC50=0.57 nM). Astressin 2B TFA blocks the protective effects mediated by CRFR2, thereby exacerbating indomethacin (HY-14397)-induced hemorrhagic intestinal injury in rats. Astressin 2B TFA reverses the protective effects of Urocortin 1 against intestinal hypermotility, bacterial invasion and upregulation of inflammatory mediators. Astressin 2B TFA also blocks the anxiogenic effect of Urocortin 2 and attenuates stress-induced anxiety-related behaviors. In the Clostridioides difficile toxin A (C. difficile toxin A)-mediated enteritis model, Astressin 2B TFA mimics the phenotype of CRFR2-deficient mice, significantly exacerbating intestinal epithelial damage, edema, neutrophil migration and the expression of multiple proinflammatory cytokines. Astressin 2B TFA is an important tool molecule for investigating the intestinal protective mechanisms of CRFR2 .
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- HY-P11303
-
|
|
CD74
MHC
|
Neurological Disease
Cancer
|
|
PADRE peptide is a pan-HLA-DR binding epitope and immunostimulant. PADRE peptide binds to the peptide-binding groove of MHC class II molecules for presentation to CD4 + T cells, thereby effectively stimulating specific immune responses. PADRE peptide not only enhances anti-tumor immune responses, inhibits tumor growth and prolongs survival; it also significantly increases the frequency of E7-specific CD8 + T cells and improves therapeutic efficacy against TC-1 tumors when used in combination with E7 peptide-based vaccines and poly (I:C). The intensity of the immune response induced by PADRE peptide is lower than that of the Ii-PADRE DNA vaccine, and it fails to enhance the immune effect of CRT-E7 DNA. PADRE peptide is widely applicable to research on related tumors such as melanoma, glioblastoma and cervical cancer .
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- HY-P1907
-
|
|
HPV
|
Cancer
|
|
Human Papillomavirus (HPV) E7 protein (49-57) is a cytotoxic T lymphocyte (CTL) epitope peptide derived from HPV16 E7 protein (sequence: RAHYNIVTF). Human Papillomavirus (HPV) E7 protein (49-57) induces E749-57-specific CTL responses. Human Papillomavirus (HPV) E7 protein (49-57) can be used for the research of cervical cancer .
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-
- HY-P11058
-
|
OVAp
|
MHC
|
Cancer
|
|
OVA(250-264) (OVAvac) (OVAp) is an antigen peptide that can be from ovalbumin (OVA) presented by the class I MHC molecule, H-2Kb. OVA(250-264) combined withαMSLN (anti-MSLN antibody) significantly induces antigen-specific CD8 + T cell generation and infiltration for enhancing antitumor efficacy in orthotopic pancreatic cancer mice model. OVA(250-264) can be used for neoantigen vaccine development in pancreatic cancer immunotherapy research .
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-
- HY-P10086
-
|
Human TREM-1(213-221)
|
TREM receptor
TNF Receptor
Interleukin Related
c-Fms
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TREM-1 inhibitory peptide GF9 (Human TREM-1 (213-221)) is a TREM-1 inhibitor. TREM-1 inhibitory peptide GF9 blocks the TREM-1 signaling pathway via a ligand-independent mechanism, spontaneously inserts into the cell membrane to dissociate TREM-1 from DAP-12, and functions through the Signaling Chain Homooligomerization (SCHOOL) model. TREM-1 inhibitory peptide GF9 reduces the levels of TNFα, IL-1β, IL-6, and M-CSF. TREM-1 inhibitory peptide GF9 inhibits tumor growth, prolongs the survival of mice with pancreatic cancer models, ameliorates collagen-induced arthritis, and exerts protective effects on bone and cartilage simultaneously. TREM-1 inhibitory peptide GF9 can be used in research related to arthritis, pancreatic cancer, retinopathy, alcoholic liver disease, and liver cancer .
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-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
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-
- HY-P5581
-
|
|
Peptides
|
Infection
Inflammation/Immunology
Cancer
|
|
Alloferon 1 is an antiviral and antitumoral peptide. Alloferon 1 stimulates natural cytotoxicity of human peripheral blood lymphocytes. Alloferon 1 also induces IFN synthesis, and enhances antiviral and antitumor resistance in mice. Alloferon 1 also shows anti-inflammatory activity in λ-carrageenan-induced paw edema model. Alloferon 1 can be isolated from the blood of the blow fly Calliphora vicina (Diptera) .
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-
- HY-P6292
-
|
|
PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
|
Neurological Disease
Cancer
|
|
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
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-
- HY-P6084
-
|
|
NOD-like Receptor (NLR)
p38 MAPK
Apoptosis
|
Inflammation/Immunology
|
|
RP-220 is a renalase peptide targeting NLRP3. RP220 has anti-inflammatory and anti-apoptotic activities. RP220 inhibits renal tubular epithelial cells apoptosis with alkaline insult by activating MAPK signaling pathway. RP220 significantly inhibits NLRP3 expression and reduces macrophage infiltration and kidney tissue damage in acute kidney injury (AKI) mice model. RP-220 can be uses for systemic lupus erythematosus (SLE) and its complication lupus nephritis (LN) research .
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-
- HY-P10109
-
|
|
Glucose-6-Phosphate Isomerase (GPI)
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
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-
- HY-P4846
-
|
|
CXCR
Apoptosis
IFNAR
TNF Receptor
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and acts as a CXCR2 agonist . Ac-Pro-Gly-Pro-OH exerts bactericidal activity by generating hydrogen peroxide, inhibits pulmonary inflammation, and reduces immune cell apoptosis (apoptosis). Ac-Pro-Gly-Pro-OH promotes the production of IFN-γ and inhibits the production of TNF-α and IL-6 in leukocytes. Ac-Pro-Gly-Pro-OH increases the survival rate of mice in sepsis models, enhances the bactericidal activity of neutrophils, acts as a neutrophil chemoattractant, induces neutrophil polarization, and regulates inflammatory and repair processes. Ac-Pro-Gly-Pro-OH induces chronic inflammation and tissue remodeling through sustained action. Ac-Pro-Gly-Pro-OH is released via alkaline hydrolysis of corneal proteins in alkali-injured eyes, thereby driving the early infiltration of neutrophils into the cornea. Ac-Pro-Gly-Pro-OH is applicable to research related to sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcer .
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-
- HY-P11005
-
|
|
Dynamin
ATP Synthase
|
Neurological Disease
|
|
P259 is a Drp1-Mff inhibitor. P259 distinguishes physiological from pathological fission by specifically inhibiting Drp1-Mff interaction. P259 elongates cell mitochondria and disrupts mitochondrial function and motility. P259 reduces ATP levels and alters mitochondrial structure in the brain, resulting in behavioral deficits in wild-type mice and a short lifespan in Huntington's disease (HD) mice model .
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-
- HY-105063
-
|
|
HSP
|
Metabolic Disease
Inflammation/Immunology
|
|
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes .
|
-
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P11060
-
|
Adpgk peptide
|
MHC
|
Cancer
|
|
MC38 SLP Adpgk (Adpgk peptide) is an H-2 K b-restricted colorectal cancer neoantigen peptide. MC38 SLP Adpgk is formulated into PCNP nanocomplexes together with CpG ODN. PCNP vaccines significantly enhance the co-delivery efficiency of neoantigens and adjuvants to lymphoid organs, and activate cytotoxic T cells. PCNP vaccines not only protect mice from MC-38 colorectal tumor invasion, but also exhibit anti-tumor efficacy in established colorectal tumor models and significantly prolong the survival of tumor-bearing mice .
|
-
- HY-P10868
-
|
RLS-0071
|
Reactive Oxygen Species (ROS)
|
Infection
Inflammation/Immunology
|
|
Pegtarazimod (RLS-0071) is a dual-target anti-inflammatory peptide that exerts its effects by simultaneously regulating the complement system and neutrophil-associated inflammatory pathways. Pegtarazimod reduces ROS production both in vitro and in vivo, and decreases the level of neutrophil elastase, a marker of neutrophil extracellular traps (NETs), in vivo, thereby alleviating inflammatory responses. Pegtarazimod significantly improves the survival rate of mice in multiple in vivo models of acute graft-versus-host disease (aGVHD). Pegtarazimod inhibits the activation of the C1 complex, reduces the herpes zoster-like spread of herpes simplex virus type 1 skin infection, and improves the survival rate of infected mice . Pegtarazimod can be used in research related to acute graft-versus-host disease, acute pulmonary diseases, and skin herpes simplex virus type 1 infection .
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-
- HY-P10792
-
|
|
EGFR
|
Cancer
|
|
HER2-targeted peptide H6F is a HER2 targeting peptide that binds to HER2 to target breast cancer cells, with the amino acid sequence YLFFVFER. The HER2-targeted peptide H6F can be conjugated with the bifunctional chelating agent hydrazinonicotinamide (HYNIC) for radiolabeling with 99mTc. Single-photon emission computed tomography (SPECT) imaging shows that the labeled HER2-targeted peptide H6F specifically accumulates in HER2-positive MDA-MBA-453 tumor-bearing mice models. The HER2-targeted peptide H6F can be used for tumor molecular imaging studies .
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-
- HY-P10427
-
|
|
CXCR
Dengue Virus
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
|
-
- HY-P5521
-
mLR12
1 Publications Verification
|
Peptides
|
Cardiovascular Disease
|
|
mLR12 is a Trem1 inhibitory peptide. mLR12 decreases aortic rupture rate in BAPN-induced Thoracic aortic aneurysm and dissection (TAAD) mice model .
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-
- HY-P11208C
-
|
|
GABA Receptor
|
Inflammation/Immunology
|
|
mNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .
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-
- HY-P5396A
-
|
|
Amino Acid Decarboxylase
|
Others
|
|
GAD65 (524-543) acetate is a biological active peptide with amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). GAD65 (524-543) acetate is one of the first fragments of the islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. GAD65 (524-543) acetate is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with GAD65 (524-543) acetate increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells .
|
-
- HY-P11287
-
|
|
Interleukin Related
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
DOTA-Pep-1L is a polypeptide formed by the conjugation of DOTA and Pep-1L. DOTA-Pep-1L specifically binds to IL13RA2 and can be used for the synthesis of targeted polypeptides. DOTA-Pep-1L yields the isotopically labeled product [ 225Ac]DOTA-Pep-1L, which exerts α-radiation killing effects on orthotopic glioma cells and extends the median survival time of mice bearing orthotopic glioma models after stereotactic injection. DOTA-Pep-1L can be used for PET imaging, tumor targeting and glioma research .
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-
- HY-P10966A
-
|
|
IKK
NF-κB
|
Inflammation/Immunology
|
|
Tat-IKIP (46-60) TFA is the trifluoroacetic acid of Tat-IKIP (46-60) (HY-P10966). Tat-IKIP (46-60) is a IκB kinase (IKK)-targeting membrane-penetrating peptide. Tat-IKIP (46-60) inhibits IKK activation and NF-κB targeted gene expression by disrupting the IKKβ/NEMO complex. Tat-IKIP (46-60) significantly reduces DSS (HY-116282)-induced acute inflammation in inflammatory bowel disease (IBD) mice model and attenuates Zymosan-induced acute arthritis in acute arthritis model (AAM). Tat-IKIP (46-60) can be used for inflammatory diseases research, such as IBD, pancreatitis and rheumatoid arthritis .
|
-
- HY-P11026
-
|
DOTA-PEG4-TMVP1446
|
VEGFR
|
Cancer
|
|
DOTA-TMVP1446 is a VEGFR-3 targeting peptide. DOTA-TMVP1446 labeled with 68Ga accurately detectes the status of lymph node metastasis, even in micrometastatic tumors, in the B16-F10 tumor mice model. DOTA-TMVP1446 can be used as a radiotracer for cancer-metastatic sentinel lymph nodes (m-SLN) imaging .
|
-
- HY-P4650
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Tyrosylhistidine is a dipeptide consisting of tyrosine and histidine (Tyr-His). Tyrosylhistidine is an orally active antihypertensive peptide. Tyrosylhistidine reduces blood pressure in mice in a model of spontaneous hypertension .
|
-
- HY-P11206A
-
|
Murine cardiac TnI peptide TFA
|
Peptides
|
Inflammation/Immunology
|
|
Murine cardiac troponin I peptide (Murine cardiac TnI peptide) TFA is a murine cardiac troponin I (cTnI) peptide. Murine cardiac troponin I peptide TFA can induce significant myocardial inflammation followed by fibrosis and heart failure with increased mortality in mice model. Murine cardiac troponin I peptide TFA can be used for heart failure research .
|
-
- HY-P11208
-
|
|
GABA Receptor
|
Inflammation/Immunology
|
|
mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA .
|
-
- HY-P10992
-
|
|
PI3K
Akt
mTOR
Caspase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research .
|
-
- HY-P11004
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
A3-APO is an antimicrobial peptide. A3-APO has a significant antimicrobial activity by a dual mode of action with both membrane disintegration and intracellular target inhibition. A3-APO can deactivate bacterial toxins and increase the expression of anti-inflammatory cytokines (such as IL-4 and IL-10), without antimicrobial resistance. A3-APO accelerates burn wounds healing in mice infection model of Acinetobacter baumannii and Staphylococcus aureus .
|
-
- HY-P10988
-
|
|
Apoptosis
MDM-2/p53
Integrin
|
Cancer
|
|
LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model .
|
-
- HY-P11018
-
|
|
Peptide-Drug Conjugates (PDCs)
Ephrin Receptor
|
Cancer
|
|
(123B9)2-L2-PTX is an EphA2-agonistic peptide-drug conjugate (PDC). (123B9)2-L2-PTX consists of a dimeric 123B9 (HY-P10579) and Paclitaxel (HY-B0015). (123B9)2-L2-PTX significantly reduces circulating tumor cells and inhibits lung tumor metastasis in breast-cancer-Metastasis mice model. (123B9)2-L2-PTX can be used for cancers research, such as melanomas and ovarian and breast cancers .
|
-
- HY-P11206
-
|
Murine cardiac TnI peptide
|
Peptides
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Murine cardiac troponin I peptide (Murine cardiac TnI peptide) is a murine cardiac troponin I (cTnI) peptide. Murine cardiac troponin I peptide can induce significant myocardial inflammation followed by fibrosis and heart failure with increased mortality in mice model. Murine cardiac troponin I peptide can be used for heart failure research .
|
-
- HY-P11262
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GUB021794 is a potent and highly selective glucagon-like peptide-1 receptor (GLP-1R) agonist developed using the streaMLine platform with an EC50 value of 18 pM. GUB021794 has a very weak activity against SCTR, with an EC50 value of 190 nM. GUB021794 can significantly reduce the body weight, food intake, and total fat mass of mice in a diet-induced obesity (DIO) model. GUB021794 can be used for research on obesity/diabetes .
|
-
- HY-P11297
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
AC-SDKP-NH2 is a substrate peptide of Angiotensin converting enzyme (ACE). AC-SDKP-NH2 has anti-inflammatory and anti-fibrotic activities. AC-SDKP-NH2 directly acts on tissues and prevents or reverses them from excessive fibrosis, but fails to reduce blood pressure and left ventricular hypertrophy (LVH). AC-SDKP-NH2 attenuates inflammation and cell differentiation, proliferation and migration, therefore reducing fibrosis in the heart, vessels and kidneys in mice model. AC-SDKP-NH2 can be used for cardiovascular diseases such as hypertension research .
|
-
- HY-P10786
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. LinTT1 peptide targets peritoneal carcinoma (PC) by binding to the p32 (gC1qR) receptor. It can conjugate with iron oxide nanoworms (NWs) to form a nanocarrier. This nanocarrier is taken up by peritoneal carcinoma cells in vitro and enters the mitochondria; it also exhibits significant tumor targeting and penetration effects in mice. Moreover, LinTT1-functionalized nanocarriers, combined with the pro-apoptotic peptide [D(KLAKLAK)2], show significant tumor suppression in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery carrier for peritoneal cancer research .
|
-
- HY-P10775A
-
|
|
MMP
|
Cancer
|
|
BT1769 acetate is a conjugate and antitumor agent targeting MT1-MMP, with a Kd value of 3.35 nM against human targets. BT1769 acetate exhibits favorable pharmacokinetic properties. BT1769 acetate specifically binds to MT1-MMP via its bicyclic peptide component, delivering the cytotoxic agent MMAE (HY-15162) to antigen-expressing cells. It effectively inhibits tumor growth, induces complete responses, and significantly prolongs event-free survival in osteosarcoma patient-derived xenograft models. BT1769 acetate shows extremely low activity in Ewing sarcoma models and can be used in osteosarcoma-related research .
|
-
- HY-P10966
-
|
|
IKK
NF-κB
|
Inflammation/Immunology
|
|
Tat-IKIP (46-60) is a IκB kinase (IKK)-targeting membrane-penetrating peptide. Tat-IKIP (46-60) inhibits IKK activation and NF-κB targeted gene expression by disrupting the IKKβ/NEMO complex. Tat-IKIP (46-60) significantly reduces DSS (HY-116282)-induced acute inflammation in inflammatory bowel disease (IBD) mice model and attenuates Zymosan-induced acute arthritis in acute arthritis model (AAM). Tat-IKIP (46-60) can be used for inflammatory diseases research, such as IBD, pancreatitis and rheumatoid arthritis .
|
-
- HY-P11075
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research .
|
-
- HY-P11028
-
|
|
CDK
|
Cancer
|
|
M1-20 is a CDK1 inhibitor. M1-20 promotes CDK1 ubiquitination by CUL4-DDB1-DCAF1 complexes and degradation through the proteasome pathway. M1-20 abolishes the formation of CDK1/CCNB1 complexes. M1-20 has significant anticancer activity of spontaneous breast cancer in FVB/N MMTV-PyVT mice model .
|
-
- HY-P10977
-
|
|
Sodium Channel
RIP kinase
|
Neurological Disease
|
|
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
|
-
- HY-P10312
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models .
|
-
- HY-P11232
-
|
|
Toll-like Receptor (TLR)
Bacterial
|
Infection
|
|
NAB815 is a specific inhibitor of the Stx2a (Kd = 0.01 μM)/TLR4 interaction. NAB815 inhibits the neutrophil/Stx2a interaction (IC50 = 0.057 μg/mL). NAB815 inhibits the formation of Stx2-containing extracellular vesicles (EVs) produced by leukocytes and platelets and reduces their toxic effects in cellular (Vero cells) and animal models (CD-1 mice). NAB815 reduces bacterial loads in the kidneys, urine, and bladders of Escherichia coli-infected mice. NAB815 is useful in the study of hemolytic uremic syndrome (HUS) .
|
-
- HY-P10109A
-
|
hG6PI (325-339) hydrochloride
|
Glucose-6-Phosphate Isomerase (GPI)
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) hydrochloride is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) hydrochloride primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) hydrochloride induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
- HY-P5875
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
- HY-P5396
-
|
|
Amino Acid Decarboxylase
|
Others
|
|
GAD65 (524-543) is a biological active peptide with amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). GAD65 (524-543) is one of the first fragments of islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. GAD65 (524-543) is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with GAD65 (524-543) increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells .
|
- HY-P4610
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
H-Trp-Tyr-OH is an orally active tryptophan-tyrosine dipeptide with blood-brain barrier permeability. H-Trp-Tyr-OH exerts physiological regulatory effects by stimulating enteroendocrine cells to secrete glucagon-like peptide GLP-1. In mouse models of tauopathies, H-Trp-Tyr-OH inhibits tau phosphorylation, reduces the level of neurofibrillary tangles, increases dopamine turnover, upregulates synapsin expression, and elevates cecal short-chain fatty acid levels, thereby improving behavioral deficits and extending lifespan. H-Trp-Tyr-OH can be used in research related to impaired glucose tolerance and tauopathies .
|
- HY-P11592
-
|
|
Bacterial
|
Infection
|
|
KIKIKPWWWPKIKIK-NH2 is a β-turn antimicrobial peptide. KIKIKPWWWPKIKIK-NH2 can inhibit bacterial biofilm formation and bind to lipopolysaccharid. KIKIKPWWWPKIKIK-NH2 shows wound-healing ability in mice bacteria-infected full-thickness wound models. KIKIKPWWWPKIKIK-NH2 can be used for the research of bacterial infection .
|
- HY-P11603
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
SK56 is a GSDMD-NT pore inhibitor. SK56 inhibits pyroptosis (Pyroptosis) and the release of pyroptosis-related cytokines in macrophages and human peripheral blood leukocytes. SK56 prevents extensive cell death in human alveolar organoids in an organoid-macrophage co-culture model. SK56 prevents death from infectious shock induced by LPS (HY-D1056) or cecal ligation and puncture in mice. SK56 can be used in studies related to sepsis .
|
- HY-P11634
-
|
|
Bacterial
|
Infection
|
|
KF-22 is an antimicrobial peptide that exhibits antimicrobial activity against both Gram-negative and Gram-positive bacteria. KF-22 demonstrates broad-spectrum, potent activity against multidrug-resistant bacteria with low toxicity. KF-22 can be used in research related to infections .
|
- HY-P11582
-
|
|
Bacterial
|
Infection
|
|
CyLip-20 is a cyclic lipopeptide antimicrobial peptide that targets Gram-positive and Gram-negative bacteria. CyLip-20 exhibits low hemolytic activity and mild in vivo toxicity. CyLip-20 disrupts the integrity of bacterial outer membrane, inner membrane and cytoplasmic membrane by binding to bacterial lipopolysaccharide (LPS), triggering membrane permeabilization, depolarization and leakage of intracellular contents, and inhibits bacterial biofilm formation. In animal models, CyLip-20 reduces the bacterial load in skin wounds of mice infected with MRSA, promotes wound healing, decreases the levels of inflammatory cytokines and reduces inflammatory cell infiltration. CyLip-20 can be used in research related to MRSA skin wound infections .
|
- HY-P11615
-
|
|
Bacterial
|
Infection
|
|
FuK is a WK2-analog antimicrobial peptide modified with fluorinated unnatural amino acids. FuK has an LD50 of 72.34 mg/kg in mice, shows no hemolytic activity, with high stability against trypsin, chymotrypsin, and saline environments. FuK exerts bactericidal effects by enhancing the permeability of bacterial outer membranes, inducing depolarization of cytoplasmic membranes, and disrupting membrane potential balance against bacterias such as Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and MRSA. FuK exhibits synergistic antimicrobial activity with polymyxin B (HY-149179), vancomycin (HY-B0671), and ciprofloxacin (HY-B0356), and also inhibits Ciprofloxacin-induced bacterial drug resistance. FuK has in vivo safety, effectively reduces bacterial load and inflammatory cell infiltration in a mouse MRSA model, and promotes collagen fiber formation in skin wounds .
|
- HY-P11773
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Integrin
|
Others
|
|
3P-RGD2 is a dimeric cyclic RGD (Arg-Gly-Asp) peptide. When radiolabeled with 99mTc, 3P-RGD2 serves as a selective radiotracer for integrin αvβ3. When radiolabeled with 99mTc, 3P-RGD2 enables single-photon emission computed tomography imaging of integrin αvβ3 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-108841
-
Raleukin
Maximum Cited Publications
52 Publications Verification
Kineret; Anakinra
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Raleukin (AMG-719) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin significantly reduces neutrophil accumulation in blood vessels and brain infarct volume as well as improves motor coordination performance in ischemic stroke mice model. Anakinra can be used to study chronic inflammatory disorders like rheumatoid arthritis and cardiovascular recurrence post-myocardial infarction .
|
-
(5)
-
- HY-P99022
-
|
R-04909832; RG-1450
|
Amyloid-β
|
Neurological Disease
|
|
Gantenerumab is a fully humanized anti-Aβ IgG1 monoclonal antibody. Gantenerumab can specifically bind to Aβ fibrils and plaques and can be used in Alzheimer's disease research .
|
-
(5)
-
- HY-P990116
-
|
|
Osteopontin
|
Inflammation/Immunology
|
|
Anti-Mouse osteopontin/SPP1 Antibody (103D6) is a mouse-derived anti-mouse osteopontin/SPP1 IgG2c κ type antibody inhibitor. Anti-Mouse osteopontin/SPP1 Antibody (103D6) increases cytotoxic T lymphocyte lytic activity and suppresses colon tumor growth. Anti-Mouse osteopontin/SPP1 Antibody (103D6) ameliorates liver injury in common bile duct ligation (CBDL)-induced primary sclerosing cholangitis mice models .
|
-
(5)
-
- HY-P990117
-
|
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
(5)
-
- HY-P99583
-
|
MEDI4893
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
|
-
(5)
-
- HY-P99216
-
|
PF-04360365; RN 1219
|
Amyloid-β
|
Neurological Disease
|
|
Ponezumab (PF-04360365; RN 1219) is a humanized anti-amyloid-β (Amyloid-β) IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves the performance of mice in various learning and memory models. Ponezumab is applicable to the research of Alzheimer's disease .
|
-
(5)
-
- HY-P991584
-
|
|
FGFR
|
Cancer
|
|
HuGAL-FR21 is a humanized antiFGFR2IIIb IgG1 monoclonal antibody. HuGAL-FR21 can block the binding of FGF2, FGF7, and FGF10 to FGFR2IIIb and inhibit FGF-induced phosphorylation of FGFR2IIIb. HuGAL-FR21 can downregulate the expression of FGFR2 in SNU-16 cells. HuGAL-FR21 shows the significant anti-tumor activity in athymic nude mice bearing gastric cancer xenograft models. HuGAL-FR21 can be used for research on cancer such as gastric cancer .
|
-
(5)
-
- HY-P99118
-
|
HLX 10
|
PD-1/PD-L1
Akt
STAT
|
Cancer
|
|
Serplulimab (HLX 10) is a humanized anti-PD-1 monoclonal antibody. Serplulimab can inhibit tumor growth, regulate the tumor microenvironment, and has anti-tumor activity. Serplulimab can be used in the research of cancer such as lung cancer and colon cancer .
|
-
(5)
-
- HY-P99148
-
|
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-Mouse TNF alpha Antibody (TN3-19.12) is an anti-mouse TNF alpha IgG antibody inhibitor derived from host Armenian Hamster. Anti-Mouse TNF alpha Antibody (TN3-19.12) neutralizes cytotoxic activity in supernatants obtained from LNC-8 cells. Anti-Mouse TNF alpha Antibody (TN3-19.12) reduces the symptoms and severity of EAE (experimental allergic encephalomyelitis) in LNC-8 cells xenograft mice models. Anti-Mouse TNF alpha Antibody (TN3-19.12) prevents diabetes in NOD mice. Anti-Mouse TNF alpha Antibody (TN3-19.12) shows apparent radiosensitizing effect in CD2F1 mice .
|
-
(5)
-
- HY-P99124
-
|
|
CD3
|
Inflammation/Immunology
|
|
Anti-Mouse CD3 Antibody (17A2) is an anti-mouse CD3 IgG2b antibody inhibitor derived from the host Rat. Anti-Mouse CD3 Antibody (17A2) enhances T-cell proliferation and activation and stimulate IFN-γ or IL-17 production in splenic T cells. Anti-Mouse CD3 Antibody (17A2) significantly suppresses mortality in Graft-versus-host disease (GVHD) mice models .
|
-
(5)
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
-
(5)
-
- HY-P991550
-
|
|
CD22
|
Cancer
|
|
RFB4 is an anti-CD22 monoclonal antibody. RFB4 can be fused with Pseudomonas aeruginosa exotoxin (PE38) via disulfide bonds to construct recombinant immunotoxins, such as RFB4 (dsFv)-PE38. RFB4 is applicable to the research of cancers including lymphoma .
|
-
(5)
-
- HY-P991228
-
|
|
Galectin
|
Cancer
|
|
LYT-200 is a humanized monoclonal antibody against galectin-9 (Galectin-9). LYT-200 binds to galectin-9 expressed on the surface of hematologic malignant cells, inhibits pro-leukemic functions and induces cell death. LYT-200 can be used in research related to hematologic malignancies .
|
-
(5)
-
- HY-P990914
-
|
GS-1811; JTX-1811
|
CCR
|
Inflammation/Immunology
Cancer
|
|
Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a KD of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstream CCR8 signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology .
|
-
(5)
-
- HY-P99922
-
|
|
LAG-3
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
(5)
-
- HY-P990107
-
|
|
TGF-β Receptor
|
Cancer
|
|
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
|
-
(5)
-
- HY-P991570
-
|
AD5-10; oba-01 Antibody
|
TNF Receptor
Apoptosis
Caspase
Atg8/LC3
Akt
Beclin1
JNK
|
Cancer
|
|
Zaptuzumab (AD5-10) is a DR5-specific humanized monoclonal antibody that selectively binds to DR5 with high affinity. Zaptuzumab specifically induces cancer cell death by both caspase-apoptosis and autophagic cell death (ACD). Zaptuzumab activates both ADCC and CDC. Zaptuzumab induces ROS generation and GSH level reduction. Zaptuzumab shows a significant suppression of the tumor growth and good safety in various xenografts mice tumor models .
|
-
(5)
-
- HY-P990953
-
|
Gen1047
|
CD3
|
Cancer
|
|
Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
|
-
(5)
-
- HY-P991609
-
|
|
MMP
|
Cancer
|
|
ABX-MA1 is a humanized IgG2 monoclonal antibody inhibitor targeting MCAM/MUC18. ABX-MA1 significantly decreases homotypic aggregation and heterotypic adhesion to HUVECs, and the formation of experimental lung metastasis. ABX-MA1 potently inhibits tumor growth, angiogenesis, and MMP-2 expression in A375SM/WM2664 xenograft mice model, promising for melanoma research .
|
-
(5)
-
- HY-P99382A
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
Vopratelimab (Mouse IgG2a) is a agonist monoclonal antibody that selectively targets Inducible CO-Stimulator of T cells (ICOS). The variable region of Vopratelimab (Mouse IgG2a) is consistent with that of Vopratelimab (HY-P99382), while the constant region is of Mouse IgG2a sequence. Vopratelimab (Mouse IgG2a) has antitumor immune response and enhances combinatorial efficacy with anti-PD-1 (HY-P9902A) therapy .
|
-
(5)
-
- HY-P990264
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4 +, CD8 + T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models .
|
-
(5)
-
- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
-
(5)
-
- HY-P990215
-
|
|
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Anti-Mouse IL-27 p28 Antibody (MM27.7B1) is a mouse-derived anti-mouse IL-27 p28 IgG2a, κ type antibody inhibitor. Anti-Mouse IL-27 p28 Antibody (MM27.7B1) can neutralize IL-27. Anti-Mouse IL-27 p28 Antibody (MM27.7B1) delays CD8+ T cell reconstitution mediated by IL-27 after murine anti-thymocyte globulin (mATG) treatment in BALB/c heart allografts mice models .
|
-
(5)
-
- HY-P990181
-
|
|
Glutathione Peroxidase
STING
|
Inflammation/Immunology
|
|
Anti-Mouse myeloperoxidase/MPO Antibody (6G4) is an anti-mouse myeloperoxidase/MPO IgG2c monoclonal antibody. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) can activate the cGAS/STING pathway. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) induces acute and chronic kidney injury in mice. Anti-Mouse myeloperoxidase/MPO Antibody (6G4) is often used in the construction of inflammation conditions models such as anti-neutrophil cytoplasmic antibody (ANCA)-associated vasculitides (AAV) .
|
-
(5)
-
- HY-P991634
-
|
|
CD73
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
IBI-325 is a humanized monoclonal antibody inhibitor targeting CD73. IBI-325 completely inhibits CD73 enzymatic activity without hook effect. IBI-325 reverses Adenosine monophosphate (HY-A0181)-mediated immune suppression and significantly inhibits T cell proliferation and cytokines (IL-2, IFN-γ and TNF-α) release. IBI-325 has potent antitumor activities in hPBMC-reconstituted mice model and hCD73 knock-in mice model. IBI-325 can be used for cancer immunotherapy research .
|
-
(5)
-
- HY-P991566
-
|
|
CTLA-4
|
Cancer
|
|
KD6001 is a humanized IgG1κ monoclonal antibody, targeting CTLA4. KD6001 significantly disrupts CTLA-4 interactions with CD80 (IC50: 16 ng/mL) and CD86. KD6001 enhances IL-2 and IFNγ expression in PHA-activated human lymphocytes and exhibits potent antitumor effects. KD6001 effectively inhibits tumor growth in MC38, B16, and Hepa1-6 tumor mice model. KD6001 can be used for cancers research, such as advanced melanoma, hepatocellular carcinoma and liver cancer .
|
-
(5)
-
- HY-P991542
-
|
|
CD19
|
Cancer
|
|
GBR-401 is a humanized anti-CD19 monoclonal antibody with high affinity for FcγRIIIa. GBR-401 exerts a potent in vitro and in vivo cytotoxic activity against various B-cell malignancies. GBR-401 induces cell death by antibody dependent cellular cytotoxicity (ADCC) and direct killing effect. GBR-401 demonstrates potent activity of depleting malignant B cells and prolongs mice survival in multiple xenograft severe combined immunodeficiency (SCID) mice models .
|
-
(5)
-
- HY-P991243
-
|
|
EGFR
Akt
|
Cancer
|
|
MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
|
-
(5)
-
- HY-P991004
-
|
LB-101
|
CD47
PD-1/PD-L1
|
Cancer
|
|
Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
|
-
(5)
-
- HY-P991595
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
HB-0017 is a humanized IgG1κ monoclonal antibody inhibitor, targeting IL-17A. HB-0017 inhibits the IL-6 secretion induced by IL-17A with an IC50 of 2.09 nM. HB-0017 significantly decreases ear thickness in Imiquimod (HY-B0180)-induced psoriasis-like mice model and alleviates inflammations in IL-17A-induced arthritis and air pouch mice model. The isotype control for the HB-0017 can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P991585
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
MORAb-028 is a humanized IgG1 monoclonal antibody inhibitor targeting GD2. MORAb-028 has a potent antitumor activity and kills GD2-expressing target cells via complement-mediated cytotoxicity (CDC). MORAb-028 significantly inhibits tumor growth in EL-4-luc xenograft mice model. MORAb-028 can be used for melanoma cancer research .
|
-
(5)
-
- HY-P991587
-
|
|
Orphan GPCR
|
Cancer
|
|
SAR-446523 is a humanized IgG1 monoclonal antibody inhibitor targeting GPRC5D. SAR-446523 significantly induces antibody-dependent cell-mediated cytotoxicity (ADCC). SAR-446523 has potent antitumor activity with improvement of mouse survival in NK humanized NOG huIL15 transgenic mice model bearing MM cells. SAR-446523 can be used for multiple myeloma (MM) research .
|
-
(5)
-
- HY-P991637
-
|
|
Ser/Thr Protease
|
Metabolic Disease
|
|
REGN7999 is a monoclonal antibody that inhibits TMPRSS6. REGN7999 inhibits TMPRSS6 activity, preventing Hemojuvelin (HJV) lysis, thereby enhancing BMP6-HJV signaling and increasing serum hepcidin. REGN7999 ameliorates iron overload and impaired erythropoiesis in a β-thalassemia mouse model by inhibiting TMPRSS6 activity. REGN7999 is indicated for research in β-thalassemia .
|
-
(5)
-
- HY-P991294
-
|
|
ADC Antibody
|
Cancer
|
|
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .
|
-
(5)
-
- HY-P991590
-
|
|
MHC
Apoptosis
JNK
Reactive Oxygen Species (ROS)
|
Cancer
|
|
1D09C3 is a fully human anti-HLA-DR monoclonal antibody. 1D09C3 induces apoptosis and cell death involving a cascade of events, including ROS generation, JNK activation, mitochondrial membrane depolarization, and AIF release from mitochondria. 1D09C3 shows potent anti-tumor activity and increases overall survival and median survival in JVM-2 cells and GRANTA-519 cells xenograft mice models. 1D09C3 can be used for the researches of cancer, such as chronic lymphocytic leukemia (CLL) .
|
-
(5)
-
- HY-P991966
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse EGFR Antibody (7A7) ia an anti-mouse EGFR monoclonal antibody proposed to be the mouse equivalent of cetuximab. Anti-Human/Mouse EGFR Antibody (7A7) fails to induce tumor regression in the HPV38 tumor model where EGFR is not expressed in mice. Anti-Human/Mouse EGFR Antibody (7A7) can be used in EGFR-expressing HPV38 tumor-related studies .
|
-
(5)
-
- HY-P991881
-
|
|
TGF-β Receptor
Hepcidin
Ferroportin
|
Cardiovascular Disease
|
|
KY1070 is a fully human anti-BMP6 antibody with a Kd of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease [1] [2].
|
-
(5)
-
- HY-P991528
-
|
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
PE0116 is a fully human CD137 agonistic monoclonal antibody generated from immunized harbor H2L2 human transgenic mice. PE0116 is a ligand block. PE0116 activates NF-κB signaling which significantly promotes T-cell proliferation and increases cytokine secretion in vitro. PE0116 exhibits robust antitumor activity in MC38 tumor model .
|
-
(5)
-
- HY-P992352
-
|
|
|
|
|
ES005 is an anti-tumor compound and LAG3 inhibitor. ES005 blocks the interactions of LAG3 with MHC-II, LSECtin and FGL1, thereby effectively reversing the LAG3-mediated inhibition of T cell activation and NFAT reporter gene expression. ES005 exhibits significant tumor growth inhibitory effects in syngeneic mouse breast tumor models using humanized LAG3 knock-in mice. ES005 can be used for breast tumor-related research .
|
-
(5)
-
- HY-P992074
-
|
IPH6501
|
CD20
Interleukin Related
|
Cancer
|
|
Zemlikafusp alfa (IPH6501) is a tetra-specific NK cell engager that targets CD20, CD16a, NKp46 and carries an IL-2 variant. Zemlikafusp alfa (IPH6501) is used in research for the treatment of relapsed/refractory B-cell non-Hodgkin lymphoma .
|
-
(5)
-
- HY-P991958
-
|
|
CTLA-4
|
Cancer
|
|
GIGA-564 is a fully human anti-CTLA4 IgG1 monoclonal antibody with a Kd of 9.8 nM. GIGA-564 binds to a unique epitope of CTLA-4, mediates FcR-dependent signaling pathways, depletes CTLA-4-highly-expressing regulatory T cells within tumors, and inhibits the proliferation of peripheral regulatory T cells. GIGA-564 exhibits anti-tumor activity in mouse models. GIGA-564 can be used for tumor research .
|
-
(5)
-
- HY-P992410
-
|
|
PAI-1
TGF-beta/Smad
|
Inflammation/Immunology
|
|
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
|
-
(5)
-
- HY-P991864
-
|
MDX-124
|
Formyl Peptide Receptor (FPR)
|
Cancer
|
|
Annexuzlimab is a humanised IgG1 monoclonal antibody which specifically binds to ANXA1 disrupting its interaction with formyl peptide receptors 1 and 2 (FPR1/2). Annexuzlimab arrests cell cycle progression with cancer cells accumulating in the G1 phase. Annexuzlimab targets secreted ANXA1, preventing FPR1/2 activation and reducing cancer progression. Annexuzlimab can be used for the research of triple negative breast cancer, pancreatic cancer and osteosarcoma .
|
-
(5)
-
- HY-P991922
-
|
|
Fc Receptor (FcR)
Complement System
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
AKIR001 is a high-affinity human IgG1 antibody targeting CD44v6. AKIR001 carries LALA-silencing mutations in its FcγR-binding domain to reduce FcγR and C1q interactions, minimizing tissue interactions and limiting CDC and ADCC risks. [ 177Lu] radiolabeled AKIR001, namely [ 177Lu]Lu-AKIR001, has anticancer activity against epidermoid carcinoma .
|
-
(5)
-
- HY-P992151
-
|
LT1002
|
LPL Receptor
Interleukin Related
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Sphingomab (LT1002) is a mouse-derived IgG1 κ monoclonal antibody and also an inhibitor targeting S1P, with high affinity for S1P and a Kd value of 0.03 ± 0.002 nM. Sphingomab blocks S1P-mediated IL-8 release in ovarian cancer cells. Sphingomab exhibits anti-angiogenic activity in a mouse model of choroidal neovascularization. Sphingomab reduces peripheral blood lymphocyte counts. Sphingomab can be used in the research of ovarian cancer and age-related macular degeneration .
|
-
(5)
-
- HY-P991883
-
|
Licartin; Metuximab; Mehuzumab
|
Apoptosis
CDK
Caspase
Bcl-2 Family
|
Cancer
|
|
Metuzumab (Licartin) is a human-mouse chimeric IgG1 monoclonal antibody targeting CD147. Metuzumab induces Apoptosis, reduces levels of Cyclin D1, full-length Caspase-3, and Bcl-2, and increases Bax expression. Metuzumab enhances the sensitivity of non-small cell lung cancer (NSCLC) cells to Gemcitabine (HY-17026). Metuzumab is applicable for research on hepatocellular carcinoma and non-small cell lung cancer [1] [2].
|
-
(5)
-
- HY-P991902
-
|
|
CD20
|
Cancer
|
|
NAV006 is an anti-CD20 antibody variant of Rituximab (HY-P9913) with a Kd of 30.5 nM to CD20. NAV006 exhibits reduced interaction with CA125 and demonstrates enhanced antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) activity. NAV006 displays antitumor activity against lymphoma and can be used in research on non-Hodgkin lymphoma .
|
-
(5)
-
- HY-P991924
-
-
(5)
-
- HY-P991896
-
|
AT14-012
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
|
-
(5)
-
- HY-P991935
-
|
|
Apoptosis
|
Cancer
|
|
ANT1034 is humanized anti-CD52 antibody. ANT1034 directs antibody dependent and complement dependent cell cytotoxicity, induces Apoptosis when cross-linked or in the presence of a cross-linking antibody. ANT1034 leads to increased survival in a SCID CD52 tumour xenograft model. ANT1034 can be used for the research of B cell malignancies .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-16561
-
-
-
- HY-B0470
-
-
-
- HY-66005
-
-
-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
Cardiovascular Disease
Structural Classification
Classification of Application Fields
Leguminosae
Glycine max (L.) merr
Plants
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Bacterial
Apoptosis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
PARP
MMP
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
NF-κB
mTOR
Lactate Dehydrogenase
CDK
Glutathione Peroxidase
SOD
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
-
- HY-N0469
-
-
-
- HY-N6972
-
-
-
- HY-N0171
-
|
|
Cardiovascular Disease
other families
Classification of Application Fields
Leguminosae
Plants
Endogenous metabolite
Glycyrrhiza uralensis Fisch.
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Apoptosis
Endogenous Metabolite
|
|
Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
-
- HY-113354
-
-
-
- HY-126477
-
-
-
- HY-128850
-
-
-
- HY-N0088
-
-
-
- HY-N1420
-
-
-
- HY-N6871
-
|
|
Infection
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
-
- HY-125833
-
-
-
- HY-N6973
-
-
-
- HY-N0217
-
-
-
- HY-W071746
-
-
-
- HY-113365
-
-
-
- HY-116330A
-
|
Hyperforin DCHA
|
Natural Products
Guttiferae
Hyperlcurn perforatum L.
Plants
Source Classification
|
TRP Channel
Calcium Channel
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
|
-
-
- HY-113308A
-
|
|
Structural Classification
Animals
Classification of Application Fields
Metabolic Disease
Disease Research Fields
Steroids
Source Classification
|
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
|
|
Taurolithocholic acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
|
-
-
- HY-W012980
-
-
-
- HY-16561R
-
|
trans-Resveratrol (Standard); SRT501 (Standard)
|
Infection
Functional Molecules
Classification of Application Fields
Sunscreen
Anti-aging
Research of Health Products
Cosmetic Research
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
Cancer
|
Reference Standards
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
|
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
-
- HY-N2345
-
-
-
- HY-N0538
-
-
-
- HY-N0745
-
-
-
- HY-N4110
-
-
-
- HY-N6967
-
-
-
- HY-N6605
-
-
-
- HY-N1420A
-
-
-
- HY-N2736
-
|
|
Flavonoids
Classification of Application Fields
Flavones
Leguminosae
Other Diseases
Phenols
Polyphenols
Plants
Vicia faba L.
Disease Research Fields
Source Classification
|
Beta-lactamase
COX
Interleukin Related
Bacterial
JNK
ERK
p38 MAPK
STAT
Apoptosis
NO Synthase
Nuclear Factor of activated T Cells (NFAT)
Lactate Dehydrogenase
Reactive Oxygen Species (ROS)
SOD
Akt
Caspase
Bcl-2 Family
|
|
3′,4′,7-Trihydroxyflavone is an orally active inhibitor of OXA-48 (IC50 = 1.89 μM) and COX-1 (IC50 = 36.37 μM). 3′,4′,7-Trihydroxyflavone exhibits antioxidant and anti-inflammatory properties, inhibiting the release of inflammatory cytokines such as IL-6, IL-8, and TNF-α. 3′,4′,7-Trihydroxyflavone inhibits H2O2-induced neuronal apoptosis and ROS accumulation, and exerts anti-neuroinflammatory effects by suppressing the JNK-STAT1 pathway. 3′,4′,7-Trihydroxyflavone exhibits antimicrobial and antibiotic-modifying activities against multidrug-resistant Gram-negative enteric bacteria. 3′,4′,7-Trihydroxyflavone inhibits RANKL-induced osteoclast formation via NFATc1. 3′,4′,7-Trihydroxyflavone activates the CREB-BDNF axis and restores scopolamine (HY-N0296)-induced memory deficits in mice .
|
-
-
- HY-N0447
-
|
|
Zingiber officinale Roscoe
Monophenols
Classification of Application Fields
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
Zingiberaceae
Cancer
|
TRP Channel
Bacterial
Apoptosis
Autophagy
STAT
PERK
EGFR
PI3K
Akt
mTOR
Caspase
MMP
|
|
8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC50 value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.
|
-
-
- HY-N0493
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Campylotropis hirtella (Franch.) Schindl.
Phenols
Polyphenols
Plants
Compositae
Inflammation/Immunology
Disease Research Fields
Source Classification
|
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
|
Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
|
-
-
- HY-B2167R
-
|
DHA (Standard); Cervonic acid (Standard)
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Disease markers
Endogenous metabolite
Cardiovascular System Disorder
Source Classification
|
Reference Standards
Endogenous Metabolite
|
|
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
|
-
-
- HY-B1350A
-
-
-
- HY-125847
-
-
-
- HY-113205
-
-
-
- HY-N0171R
-
|
β-Sitosterol (Standard); 22,23-Dihydrostigmasterol (Standard))
|
Cardiovascular Disease
other families
Classification of Application Fields
Leguminosae
Plants
Endogenous metabolite
Glycyrrhiza uralensis Fisch.
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Reference Standards
Apoptosis
Endogenous Metabolite
|
|
Beta-Sitosterol (Standard) is the analytical standard of Beta-Sitosterol. This product is intended for research and analytical applications. Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
|
-
-
- HY-N0120
-
|
(E/Z)-Piceid
|
Structural Classification
Stilbenes
Classification of Application Fields
Polygonaceae
Reynoutria japonica Houtt.
Phenols
Polyphenols
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Drug Isomer
|
|
(E/Z)-Polydatin ((E/Z)-Piceid) is a mixture of the E/Z configurations of Polydatin (HY-N0120A). Polydatin can be isolated from Polygonum cuspidatum, grapes, peanuts, red wine, hop pellets, cocoa-containing products and chocolate products. Polydatin exhibits multiple biological properties, such as anti-platelet aggregation, anti-low-density lipoprotein oxidation, cardioprotective activity, anti-inflammatory and immunomodulatory functions. Polydatin shows favorable cytotoxic effects against various tumor cell lines, including cervical cancer cells, liver cancer cells, and nasopharyngeal carcinoma cells .
|
-
-
- HY-120692
-
-
-
- HY-19480
-
-
-
- HY-N6257
-
-
-
- HY-N0430
-
|
Coptisin
|
Alkaloids
Structural Classification
Classification of Application Fields
Coptis chinensis Franch.
Ranunculaceae
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-N14001
-
|
|
Structural Classification
Alkaloids
Marine natural products
Sponge
Imidazole Alkaloids
Source Classification
|
TNF Receptor
Interleukin Related
Arginase
PD-1/PD-L1
|
|
Naamidine J is an imidazole-type alkaloids discovered in a sponge. Naamidine J inhibits inflammation by binding to the protein CSE1L (KD = 5.41 μM). Namidine J significantly inhibits the expression of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6, and upregulates anti-inflammatory factors such as CD206 and Arg-1. Namidine J inhibits PD-L1 and shows antitumor activity. Namidine J significantly reduces pulmonary tissue edema, inflammatory cell infiltration and cytokine storm in mice. Namidine J can be used for the research on the immune microenvironment of acute lung injury and tumors .
|
-
-
- HY-N4107
-
-
-
- HY-116330
-
-
-
- HY-N0469R
-
|
|
Structural Classification
Microorganisms
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
Virus Protease
HSV
|
L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
|
-
-
- HY-N6893
-
|
|
Phyllodium pulchellum (L.) Desv.
Structural Classification
Classification of Application Fields
Ketones, Aldehydes, Acids
Plants
Compositae
Inflammation/Immunology
Disease Research Fields
Piptanthus nepalensis (Hook.) D. Don
Source Classification
|
NF-κB
NOD-like Receptor (NLR)
Apoptosis
Autophagy
|
Ergolide is an orally active dual inhibitor targeting NF-κB/p65 and NLRP3. Ergolide blocks the NF-κB signaling pathway and the nuclear translocation of p65, and irreversibly binds to the NACHT domain of NLRP3 to inhibit inflammasome assembly. Ergolide significantly reduces the production of inflammatory mediators (e.g., NO, PGE2) and cytokines, induces cancer cell apoptosis, autophagy and ROS generation. Ergolide also enhances the anti-tumor effect of vincristine. Ergolide alleviates acute lung injury via an NLRP3-dependent mechanism, and effectively improves the survival rate and behavioral function of septic mice and inflammatory zebrafish models. Ergolide is used in the research of metastatic uveal melanoma, neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease), sepsis and acute lymphoblastic leukemia .
|
-
-
- HY-125938
-
|
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Triterpenes
Monophenols
other families
Classification of Application Fields
Terpenoids
Phenols
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
|
|
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity Kd = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .
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- HY-112817
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8-Oxo-Deoxyguanosine triphosphate
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Microorganisms
Source Classification
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Apoptosis
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8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
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- HY-W012980R
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- HY-N1420AR
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L-Rhamnose monohydrate (Standard)
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Structural Classification
Microorganisms
other families
Plants
Saccharides
Monosaccharides
Source Classification
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Reference Standards
Endogenous Metabolite
MMP
Interleukin Related
PKA
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Rhamnose monohydrate (Standard) is the analytical standard of Rhamnose monohydrate (HY-N1420A). Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
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- HY-N16374
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Microorganisms
Antibiotics
Source Classification
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Antibiotic
Bacterial
Fungal
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Mazethramycin B (Compound II) is an antitumor antibiotic. Mazethramycin B can be isolated from the Streptomyces thioluteusM ME561-L4. Mazethramycin B has a broad-spectrum antimicrobial activity (such as MICs of 1.56 and 6.25 μg/mL for the bacteria Bacillus subtilis PCI 219 and the fungus Candida pseudotropicalis, resepectively). Mazethramycin B significantly increases survival in L1210 leukemia mice model .
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- HY-N7394
-
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(3S)-Zuonin A
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Natural Products
Virola surinamensis (Rol. ex Rottb.) Warb.
Myristicaceae
Plants
Source Classification
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AMPK
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Galbacin ((3S)-Zuonin A), the epimer of (-)-Zuonin A (HY-N7394A), is a AMPK activator. Galbacin can be isolated from Myristica fragrans (nutmeg). Galbacin stimulates AMPK enzyme in differentiated C2C12 cells. Galbacin also has anticancer activity, and inhibits the proliferation of lymphocyte and tumor cells. Galbacin prevents weight gain in diet-induced mice model. Galbacin can be used for metabolic syndrome (including obesity and type-2 diabetes) and caners research .
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- HY-D0186R
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|
Structural Classification
Natural Products
Immune System Disorder
Microorganisms
Disease markers
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
Thymidylate Synthase
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2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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- HY-113308AR
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|
Structural Classification
Animals
Steroids
Source Classification
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Reference Standards
Calcium Channel
Ferroptosis
PI3K
Reactive Oxygen Species (ROS)
Akt
HBV
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Taurolithocholic acid (sodium salt) (Standard) is the analytical standard of Taurolithocholic acid (sodium salt). This product is intended for research and analytical applications. Taurolithocholic acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-W071746R
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-
- HY-N3312R
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-
- HY-125833R
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-
- HY-N6967R
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|
(-)-α-Bisabolol (Standard)
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Plants
Source Classification
|
Reference Standards
Apoptosis
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Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
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- HY-N0976
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-
- HY-N6972R
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|
|
Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
|
Autophagy
Reference Standards
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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- HY-N16371
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Microorganisms
Ketones, Aldehydes, Acids
Source Classification
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Endogenous Metabolite
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6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid (Compound MC-1), an isocoumarin, is a metabolite of Cytogenin (HY-19606). 6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid has anti-angiogenic activity in S-180 implanted dorsal air sac mice model. 6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid also modifies collagen-induced arthritis. 6-Methoxy-8-hydroxyisocoumarin-3-carboxylic acid can be used for cancers and inflammatory diseases research .
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- HY-N1149
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- HY-113354R
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-
- HY-128850R
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- HY-N11872
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Paeonia lactiflora Pall.
Phenols
Polyphenols
Plants
Paeoniaceae
Source Classification
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Others
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Suffruticosol A is a neuroprotective agent that restores scopolamine-induced cellular neurodegenerative damage. Suffruticosol A ameliorates hippocampal cholinergic deficits and partially enhances BDNF signaling. Suffruticosol A has neuromodulatory effects in a Scopolamine (HY-N0296)-induced model, restoring memory and cognitive performance in mice. Suffruticosol A can be isolated from seeds of P. lactiflora .
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- HY-129133
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Vitis vinifera cv. Zalema
Phenols
Plants
Vitaceae
Source Classification
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Drug Isomer
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cis-Miyabenol C is an isomer of the resveratrol trimer Miyabenol C, which can be isolated from grape herbs. Miyabenol C is an inhibitor of β-amyloid (Aβ) and amyloid β precursor protein (APP) in Alzheimer's disease model mice, and inhibit β-secretase activity without changing the protein level of β-secretase BACE1 .
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- HY-N0088R
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-
- HY-126477R
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-
- HY-N0469A
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-
- HY-N12087
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-
- HY-N0918R
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-
- HY-N4107R
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-
- HY-N2345R
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- HY-116330AR
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Hyperforin DCHA (Standard)
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Structural Classification
Natural Products
Guttiferae
Hyperlcurn perforatum L.
Plants
Source Classification
|
Reference Standards
TRP Channel
Calcium Channel
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Hyperforin dicyclohexylammonium salt (Standard) is the analytical standard of Hyperforin dicyclohexylammonium salt. This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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- HY-N16465
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Phenols
Polyphenols
Plants
Lauraceae
Lindera glauca (Siebold & Zucc.) Blume
Source Classification
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Apoptosis
Reactive Oxygen Species (ROS)
STAT
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Cinnamtannin D1 is an orally active polyphenolic compound with immunosuppressive activity. Cinnamtannin D1 regulates the balance of Th17/Treg cells by inhibiting AHR expression. Cinnamtannin D1 reduces apoptosis and ROS in INS-1 cells and primary cultured murine islets induced by Palmitic acid (PA) (HY-N0830). Cinnamtannin D1 reduces Th17 cell differentiation via downregulating p-STAT3/RORγt and promotes Treg cell differentiation via upregulating p-STAT5/Foxp3. Cinnamtannin D1 exerts excellent anti-arthritic efficacy in collagen-induced arthritis (CIA) model of mice. Cinnamtannin D1 can be used for the study of rheumatoid arthritis (RA) .
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- HY-N0493R
-
|
|
Structural Classification
Flavonoids
Flavones
Campylotropis hirtella (Franch.) Schindl.
Phenols
Polyphenols
Plants
Compositae
Source Classification
|
Reference Standards
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
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Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
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- HY-N19281
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-16561S
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Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-113354S
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Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-113308S1
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Taurolithocholic acid-d4 is deuterium labeled Taurolithocholic acid. Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-16561S1
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Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-113308AS1
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Taurolithocholic Acid-d5 (sodium) is the deuterium labeled Taurolithocholic acid sodium salt. Taurolithocholic Acid sodium salt is an orally active bile acid and antiviral agent. Taurolithocholic Acid sodium salt upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic Acid sodium salt also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic Acid sodium salt serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic Acid sodium salt shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic Acid sodium salt not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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-
- HY-175318S
-
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p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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- HY-N3312S
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Matairesinol-d6 is the deuterium labeled Matairesinol. Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
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-
- HY-109120S
-
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Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-109120S1
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Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-W012481S
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Nirvanol-d5 (Ethylphenylhydantoin-d5) is deuterium labeled Nirvanol (HY-W012481) . Nirvanol (Ethylphenylhydantoin) is a metabolite of Mephenytoin (HY-B1184) that exerts anticonvulsant effects in the maximal electroshock (M.E.S.) seizure model in mice. Nirvanol shows potential for research in epilepsy-related neurological disorders .
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- HY-113354S1
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Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-W017540S
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Cyclocreatine- 13C3 is the 13C-labeled Cyclocreatine (HY-W017540). Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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-
- HY-W767399
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8-Bromo-2'-deoxyguanosine- 13C, 15N2 is the 13C- and 15N-labeled 8-Bromo-2'-deoxyguanosine (HY-W011168). 8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
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- HY-W768347
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Xylitol- 13C5 (Xylite- 13C5) is the 13C-labeled Xylitol (HY-N0538). Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-113308AS
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Taurolithocholic acid-d4 (sodium) is the deuterium labeled Taurolithocholic acid (sodium salt). Taurolithocholic acid sodium is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-113308AS2
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Taurolithocholic acid-d4-1 (sodium) is the deuterium labeled Taurolithocholic acid. Taurolithocholic acid sodium is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid sodium also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid sodium serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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-
- HY-113308S
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Taurolithocholic acid-d5 is deuterium labeled Taurolithocholic acid. Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis .
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- HY-W142432S
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Perfluoroundecanoic acid- 13C7 is the 13C-labeled Perfluoroundecanoic acid (HY-W142432). Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation .
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-
| Cat. No. |
Product Name |
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Classification |
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- HY-139659
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PROTAC Synthesis
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ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-159102
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Azide
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PVP-037.2 is a TLR7/8 agonist. PVP-037.2 can serve as an adjuvant to enhance vaccine-induced TH1 type immune responses, increasing the production of antigen-specific antibodies IgG1 and IgG2c .
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- HY-175201
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Azide
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pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
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- HY-181849
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Alkynes
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MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma .
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| Cat. No. |
Product Name |
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Classification |
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- HY-N0171A
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β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
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Cholesterol
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Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
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- HY-153808
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Adjuvant
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Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
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- HY-N0171
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Cholesterol
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Beta-Sitosterol (purity≥80%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
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- HY-N0538
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Xylite
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Fillers
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Xylitol can be classified as a polyol and sugar alcohol, exhibiting inhibitory activity on cancer cell proliferation. It induces autophagy (Autophagy) and cell death in A549 cells by activating the autophagy signaling pathway, as evidenced by the increased expression of LC3-II and Atg5-Atg12 upon Xylitol treatment. Additionally, Xylitol inhibits acetaldehyde production by Candida species, thereby reducing their carcinogenic potential. In vivo, Xylitol induces alterations in the gut microbiota of mice, which may enhance cholesterol accumulation and upregulate hepatic ChREBP, while also slowing tumor growth in the B16F10 melanoma C57BL/6 mouse model .
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- HY-W011168
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Nucleoside Analogs
Guanosine
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8-Bromo-2'-deoxyguanosine is an inflammation-related DNA halogenated adduct and an early biomarker of inflammation-induced oxidative tissue damage. The formation of 8-Bromo-2'-deoxyguanosine precedes that of oxidative and nitrative products, and it can be generated via the MPO-H2O2-Cl --Br - system. 8-Bromo-2'-deoxyguanosine serves as the immunogen for preparing the monoclonal antibody mAb8B3, which can be used to detect early DNA modifications in preclinical models; its urinary level also increases significantly in inflammatory disease models. 8-Bromo-2'-deoxyguanosine can also be produced in the dermis of UV-B irradiated mice, and the extract of Coprinus comatus significantly reduces its level. 8-Bromo-2'-deoxyguanosine finds applications in studies related to inflammatory diseases, diabetes, hepatocellular carcinoma, and UV-B induced skin inflammation .
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- HY-172699
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Pegylated Lipids
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DSPE-PEG2000-ANG is a conjugate of DSPE-PEG2000-MAL and Angiopep-2. Angiopep-2 is a peptide ligand that targets LRP-1. DSPE-PEG2000-ANG is used to synthesize gadolinium-boron bifunctionalized lipid nanoparticles BPA-F&DOTA-Gd@LIPO-ANG with blood-brain barrier and glioma targeting properties .
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- HY-155887
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DSPE-PEG-NH2, MW 3400 ammonium
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Pegylated Lipids
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DSPE-PEG-Amine (DSPE-PEG-NH2), MW 3400 ammonium is an amino-functionalized PEGylated phospholipid. It serves not only as a key component for preparing σ receptor-targeted liposomes (such as anisamide-modified lipids) but also as a starting material for synthesizing click chemistry- and tumor-targeted lipids including DSPE-PEG-DBCO (HY-155788) and DSPE-PEG2000-TCO (HY-170704). DSPE-PEG-Amine, MW 3400 ammonium effectively modulates the ζ potential of nanoparticles, enables complexation with nucleic acids or proteins to protect DNA from nuclease degradation, and supports ligand conjugation on the nanoparticle surface. It is used in studies related to DU-145 tumors, breast cancer, and other relevant research .
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- HY-153834
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Aptamers
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GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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- HY-177406
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Aptamers
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VR11 aptamer is a DNA-based TNF-α inhibitor with a KD of 7.0 nM. VR11 aptamer prevents TNFα-induced apoptosis and NO production. VR11 aptamer has non-immunogenicity and does not raise immune responses when injected intraperitoneally into C57BL/6 mice model. VR11 aptamer can be used for inflammatory diseases research .
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- HY-171953
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Cationic Lipids
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THP1 Lipid is an ionizable lipidoid. THP1 Lipid can be used to synthesize lipid nanoparticles (LNPs) for delivering mRNA to muscles with minimal toxicity and editing genes in specific liver tissues in tdTomato transgenic mice model. THP1 Lipid can be used for vaccine delivery and CRISPR/Cas9-mediated gene editing research .
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- HY-153834A
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Aptamers
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GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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- HY-169480
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Cationic Lipids
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Lipid C2 is an ionizable cationic lipid that has been used in the formation of lipid nanoparticles (LNP) for mRNA delivery in vivo. LNPs containing Lipid C2 and encapsulating an mRNA reporter selectively accumulate in the liver and spleen but not the heart, lungs, or kidneys in mice. LNP containing Lipid C2 and encapsulating mRNA encoding the Epstein-Barr virus (EBV) protein latent membrane protein 2 (LMP-2), in combination with an anti-programmed cell death protein 1 (PD-1) antibody, decrease tumor volume and reverse T cell exhaustion, as well as increase the percentage of CD3 +CD8 + central and CD3 +CD8 + effector memory T cells and decrease the percentage of CD3 + T cells expressing Pd-1, in the spleen in a CT26 murine EBV-infected colon cancer model .
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- HY-177933
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Aptamers
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mNOX-E36 is a murine-specific analogue of NOX-E36 (HY-148100), an anti-CCL-2 L-RNA aptamer that binds and neutralises the mouse chemokine CCL-2. mNOX-E36 reduces scarring in an experimental murine model of glaucoma filtration surgery (GFS). mNOX-E36 ameliorates lupus nephritis in mice. mNOX-E36 can be used for GFS and lupus nephritis research .
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- HY-169478
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Cationic Lipids
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Lipid N2-3L is an ionizable cationic lipid (pKa = 8.99) that can be used to generate supramolecular lipid nanoparticles (SMLNPs) for mRNA delivery. Lipid nanoparticles formed by encapsulating a luciferase reporter gene with Lipid N2-3L were detected to accumulate in the lymph nodes of mice, indicating that they can effectively enter the mouse immune system. Lipid nanoparticles formed by encapsulating ovalbumin mRNA and the TLR7/8 agonist Resiquimod (HY-13740) with Lipid N2-3L were able to reduce tumor volume and increase survival in the MC-38-OVA mouse colon cancer model. Lipid N2-3L can be used in the research of drug delivery for cancer-related therapies .
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- HY-112817A
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8-Oxo-Deoxyguanosine triphosphate trisodium
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Nucleotide Analogs
Guanine Nucleotide
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8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP trisodium solution (100mM) acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP trisodium solution (100mM) causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP trisodium solution (100mM) in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP trisodium solution (100mM) is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107202GL
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Poly(I:C) (GMP Like)
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Toll-like Receptor (TLR)
PKD
HSP
Bcl-2 Family
Interleukin Related
Apoptosis
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Infection
Inflammation/Immunology
Cancer
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Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis .
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- HY-16561G
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trans-Resveratrol; SRT501
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DNA/RNA Synthesis
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Keap1-Nrf2
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Infection
Inflammation/Immunology
Cancer
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Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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