Search Result
Results for "
binding models
" in MedChemExpress (MCE) Product Catalog:
6
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N0830
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- HY-N0830B
-
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Environmental Pollutants
Endogenous Metabolite
HSP
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Cancer
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Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
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- HY-16261
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INNO-206; DOXO-EMCH
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Topoisomerase
ADC Payload
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Cancer
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Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-11079
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Sodium Channel
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Neurological Disease
Inflammation/Immunology
Cancer
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A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter .
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- HY-D0846
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Biochemical Assay Reagents
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Neurological Disease
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Diethyl pyrocarbonate is a potent, orally active, non-specific chemical inhibitor of RNase. Diethyl pyrocarbonate has been useful in vitro as an agent relatively specific for binding to imidazole of histidine. Diethyl pyrocarbonate inhibits central chemosensitivity in rabbits. Diethyl pyrocarbonate can modify Ser, Thr, His and Tyr residues. Diethyl pyrocarbonate can be used for modeling .
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- HY-122611A
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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- HY-P9964
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11F8; IMC-11F8; LY3012211
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EGFR
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Cancer
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Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
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- HY-NP006
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SPA
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Endogenous Metabolite
Apoptosis
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Inflammation/Immunology
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Protein A (SPA) is an immunoglobulin (Ig)-binding protein that exists on the bacterial surface and can be freely secreted into the extracellular environment. Protein A blocks opsonophagocytosis and induces B cell apoptosis in vitro by binding to the Fc region of antibodies and the Fab region of B cell receptors. Protein A can form toxic immune complexes with IgG, thereby inducing leukocyte necrosis. Protein A contributes to the virulence expression of Staphylococcus aureus. Protein A triggers allergic reactions in IgG-pretreated mouse models. Protein A can be used in studies related to immune system diseases .
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- HY-B0027
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Antibiotic
Bacterial
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Infection
Metabolic Disease
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Valnemulin hydrochloride is an orally effective truncated pleurotin antibiotic that inhibits protein synthesis in bacteria by binding to peptidyl transferase in the 50s ribosome subunit. Valnemulin hydrochloride effectively eliminates Mycobacterium bovis in the lungs in an experimental bovine model of Mycoplasma bovis infection. Valnemulin hydrochloride can reduce the mortality of epidemic rabbit enteropathy and has no adverse effect on the growth performance of rabbits .
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- HY-B1864A
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Ksg hydrochloride
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Environmental Pollutants
Antibiotic
Bacterial
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Infection
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Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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- HY-P99171
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Interleukin Related
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Inflammation/Immunology
Cancer
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Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
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- HY-107830
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Endogenous Metabolite
Collagen
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Infection
Metabolic Disease
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Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
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- HY-P991577
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DS-8895A
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Ephrin Receptor
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Cancer
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DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with 89Zr, 111In, or 125I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo. .
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- HY-W008270
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γ-Crotonolactone
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Endogenous Metabolite
Bacterial
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Infection
Neurological Disease
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2(5H)-Furanone (γ-Crotonolactone) is an endogenous metabolite. 2(5H)-Furanone mimics N-acyl homoserine lactone signals, occupies the binding site of LuxR homologs, and interferes with quorum sensing-mediated gene regulation. 2(5H)-Furanone inhibits quorum sensing mediated by AHLs with different acyl chain lengths. 2(5H)-Furanone inhibits biofilm formation of environmental Aeromonas hydrophila strains on polystyrene plates. 2(5H)-Furanone suppresses spike-and-wave discharges in a rat model of generalized absence seizures and exhibits selective activity against absence seizures. 2(5H)-Furanone can be used in studies related to bacteria infections and generalized absence seizures.
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- HY-B1864B
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Ksg hydrochloride hydrate
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Antibiotic
Bacterial
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Infection
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Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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- HY-P3732
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Integrin
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Cancer
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RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models .
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- HY-103423
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Dopamine Receptor
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Neurological Disease
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PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists .
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- HY-144549
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LXR
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Cardiovascular Disease
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LXR (Liver X receptor) agonist 1 is potent LXR agonist with AC50s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis .
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- HY-P5542
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SB-01; Peniel 2000
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Factor Xa
TGF-beta/Smad
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Inflammation/Immunology
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Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases .
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- HY-P99249
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Pogalizumab; MOXR 0916
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Orexin Receptor (OX Receptor)
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Cancer
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Vonlerolizumab (Pogalizumab; MOXR 0916) is a humanized IgG1 monoclonal antibody targeting OX40 (CD134). Pogalizumab partially blocks the interaction between OX40 and its natural ligand OX40L upon binding, thereby activating the NF-κB signaling pathway. Pogalizumab enhances T cell activation and proliferation and has shown antitumor activity in mouse models .
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- HY-116940
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Sm4
1 Publications Verification
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Oct3/4
Notch
STAT
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Cancer
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Sm4 is a selective and orally active SOX18 inhibitor. Sm4 inhibits SOX18-DNA binding (IC50 = 97.5 μM); Sm4 disrupts the SOX18-RBPJ protein-protein interaction (IC50 = 42.3 μM). Sm4 blocks SOX18 DNA binding, disrupts multiple SOX18 protein-protein interactions with RBPJ, DDX1, DDX17, ILF3, SOX7 and STAT1, modulates SOX18 chromatin binding dynamics. Sm4 exerts anti‑angiogenic and anti‑lymphangiogenic effects, reduces tumor vascular density, triggers vascular defects in zebrafish, prolongs survival in mouse metastatic cancer models. Sm4 can be used for the research of breast cancer .
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- HY-P10943
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Fluorescent Dye
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Inflammation/Immunology
Cancer
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APO-15 is a phosphatidylserine-binding fluorescent probe and apoptosis imaging reagent. APO-15 exhibits high chemical stability under proteolytic and oxidative conditions, enables quantification and imaging of drug-induced apoptosis in preclinical mouse models, and is applicable to fixed tissue samples and multiple in vivo administration routes (Ex = 488 nm; Em = 525 nm). APO-15 can be used in studies related to acute lung injury and breast cancer .
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- HY-16999
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
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- HY-112316
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Epigenetic Reader Domain
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Cancer
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BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
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- HY-100982
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trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA
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GABA Receptor
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Neurological Disease
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(E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models .
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- HY-12168
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BAY 12-9566
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MMP
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Cancer
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Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
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- HY-168366
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Opioid Receptor
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Neurological Disease
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R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC50=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats .
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- HY-122255
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mGluR
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Neurological Disease
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LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
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- HY-153165
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RAR/RXR
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Others
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RXR antagonist 5 (compound 22) is a selective retinoic acid X receptor (RXR) antagonist with binding potential to RXR evaluated by modeling.
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- HY-177506
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Cholecystokinin Receptor
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Metabolic Disease
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FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research .
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- HY-122611
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Androgen Receptor
Apoptosis
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Cancer
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CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-139046
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Adrenergic Receptor
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Neurological Disease
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MEPB is a modulator of AF-2 of the androgen receptor. MEPB increases co-repressor binding of AR. MEPB can bind to the BF3 pocket of AR specifically, thereby modulating the binding of co-regulators to the AF2 domain. MEPB alleviates degeneration in spinal bulbar muscular atrophy mouse model .
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- HY-115527
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SHP2
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Cancer
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SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC50 value for SHP2 WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers .
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- HY-106969A
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Glycine Receptor (GlyR)
iGluR
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Cardiovascular Disease
Neurological Disease
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ZD 9379 sodium is a competitive glycine/NMDA receptor antagonist, with an IC50 value of 75 nM (glutamate site). ZD 9379 sodium selectively antagonizes the glycine binding site (GlyB site) on the NMDA receptor, inhibiting the binding of glycine to the NMDA receptor and alleviating excitotoxicity. ZD 9379 sodium reduces the frequency of cortical spreading depression (SDs), alleviates energy depletion in the ischemic penumbra, and delays the expansion of infarction. ZD 9379 sodium reduces the infarct volume and improves neurological function in mouse models. ZD 9379 sodium can be used in studies of acute ischemic stroke, etc .
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- HY-W127458
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Hexadecanoic acid, tin(2+) salt
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Environmental Pollutants
Endogenous Metabolite
HSP
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Neurological Disease
Metabolic Disease
Cancer
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Tin(II) palmitate (Hexadecanoic acid, tin(2+) salt) is a long-chain saturated fatty acid commonly found in animals and plants. Tin(II) palmitate can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granular cells. Tin(II) palmitate can be used to establish a model of cellular steatosis.
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- HY-P11354
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TGF-β Receptor
Apoptosis
Interleukin Related
Integrin
Cadherin
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Inflammation/Immunology
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THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis .
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- HY-175250
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TNF Receptor
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Inflammation/Immunology
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TNF-α-IN-25 is an orally active TNF-α inhibitor. TNF-α-IN-25 shows Fluorescence Polarization (FP) assay IC50 of 103 nM in FP binding assays and L929 assay IC50 of 505 nM in cell-based assays. TNF-α-IN-25 inhibits paw swelling in the glucose-6-phosphate isomerase (GPI) arthritis model. TNF-α-IN-25 can be used for the study of arthritis .
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- HY-181846
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DNA/RNA Synthesis
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Neurological Disease
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nTRD22 is an RNA-binding allosteric modulator targeting TDP-43. nTRD22 binds to the N-terminal domain of TDP-43, thereby allosterically regulating the RNA-binding domain of TDP-43 and reducing its RNA-binding ability. nTRD22 decreases the TDP-43 protein level in primary motor neurons. nTRD22 alleviates motor dysfunction in amyotrophic lateral sclerosis models. nTRD22 is applicable to related research on amyotrophic lateral sclerosis .
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- HY-W841438
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Amyloid-β
Tau Protein
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Neurological Disease
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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-16261C
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INNO-206 hydrochloride; DOXO-EMCH hydrochloride
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Topoisomerase
ADC Payload
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Cancer
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Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-177021
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Microtubule/Tubulin
Apoptosis
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Cancer
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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 .
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- HY-124483
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Arrestin
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Metabolic Disease
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W2476 is a regulator of thioredocin-interacting protein signaling pathway. W2476 promotes competitive binding of forkhead box O1 transcription factor (FOXO1). W2476 can ameliorate β-cell dysfunction and enhance insulin secretion in diabetic mouse model .
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- HY-P991618
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Transmembrane Glycoprotein
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Cancer
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ST2485 is a monoclonal antitenascin antibody. ST2485 shows additivity in tenascin C binding in vitro as well as in a xenograft model. ST2485 binds human tenascin at an epitope partially shared with BC2. ST2485 cross-reacts with murine tenascin. ST2485 can be studied in antitumor research .
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- HY-112316A
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Epigenetic Reader Domain
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Cancer
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(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome .
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- HY-126336
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Calcium Channel
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Cardiovascular Disease
Neurological Disease
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HM12 is a covalent inhibitor of L-/T-type calcium channels. HM12 can strongly inhibit the Cav1.2 (L-type) and Cav3.2 (T-type) calcium channels, and has selectivity for the N-type channels. HM12 produces an irreversible inhibition that persisted after washout. HM12 can be used to study diseases such as hypertension, pain, epilepsy, etc .
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- HY-15350
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LY 300046 hydrochloride
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Reverse Transcriptase
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Others
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Trovirdine hydrochloride, a phenethylthiazolylthiourea (PETT) derivative, is an HIV reverse transcriptase (RT) non-nucleoside inhibitor (NNI). A novel computer model of the RT/NNI binding pocket revealed spatial gaps around Trovirdine hydrochloride's pyridyl ring. Docking studies suggested that replacing this planar ring with a nonplanar piperidinyl or piperazinyl ring could better occupy the binding pocket, enhancing anti-HIV activity. Synthesized heterocyclic compounds based on this modification demonstrated greater potency than Trovirdine hydrochloride, effectively inhibiting HIV replication at nanomolar concentrations without cytotoxicity in infected peripheral blood mononuclear cells .
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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-123928
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- HY-P11354A
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TGF-β Receptor
Apoptosis
Interleukin Related
Integrin
Cadherin
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Inflammation/Immunology
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THR-123 TFA is an orally active ALK3 peptide agonist. THR-123 TFA has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 TFA suppresses inflammation, Apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 TFA can be used for the study of kidney fibrosis .
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- HY-170764
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YAP
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Cancer
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M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
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- HY-P10793
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EGFR
Apoptosis
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Cancer
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Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
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- HY-179391
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Telomerase
Apoptosis
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Cancer
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Telomerase-IN-9 is a potent and selective telomerase inhibitor. Telomerase-IN-9 significantly reduces telomerase activity by binding to hTERT, leading to decreased telomerase function. Telomerase-IN-9 induces apoptosis and inhibits colony formation. Telomerase-IN-9 reduces tumor burden, restores antioxidantbalance, and preserves lung architecture in a Benzo[a]pyrene (HY-107377)-induced lung cancer mouse model. Telomerase-IN-9 can be used for the research of lung cancer .
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- HY-103513
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GABA Receptor
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Others
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GABAA receptor agent 2 (compound 13) is a compound used to study the structure and orthosteric ligand binding of GABA(A) receptors. The relevant model of GABAA receptor agent 2 can be used to understand the details of orthosteric ligand binding, and a detailed binding mode hypothesis was created through structure-activity relationships with two homologous series of orthosteric GABA(A)R antagonists.
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- HY-106469
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MY-117
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Drug Derivative
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Neurological Disease
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Taltrimide (MY-117), a lipophilic derivative of Taurine (HY-B0351), strongly inhibits the sodium-independent binding of Taurine to synaptic membranes of brain, the effects on the binding of GABA being less pronounced. Taltrimide exhibits definitive anticonvulsive effects in experimental epilepsy models .
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- HY-P10010
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Galectin
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Cancer
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DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .
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- HY-14297
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Adrenergic Receptor
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Endocrinology
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Milveterol is a long-acting β(2)-adrenoceptor agonist with high binding activity. Milveterol exhibits high potency in vitro and a prolonged duration of action in a guinea pig bronchoprotection model. Milveterol has been structurally optimized to show enhanced binding potency compared to its parent monomer .
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- HY-148705
-
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SARS-CoV
|
Infection
|
|
Isomitomycin A is a potential inhibitor against SARS-CoV-2. Isomitomycin A targets to the hACE2 binding site of the modelled surface glycoprotein of SARS-CoV-2. Isomitomycin A can be used in studies of COVID-19 .
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-
- HY-119005A
-
-
- HY-117862
-
|
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Prostaglandin Receptor
|
Inflammation/Immunology
|
|
TASP0412098 is an orally available, potent and selective CRTH2/DP2 antagonist with high binding affinity (IC50 2.1 nM) and functional activity (IC50 12 nM). TASP0412098 has the potential to suppress asthma in mouse and guinea pig bronchial asthma models .
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-
- HY-N0830A
-
|
|
HSP
Endogenous Metabolite
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
|
Palmitic acid calcium is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid calcium is used to establish a cell steatosis model .
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-
- HY-101119
-
|
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Estrogen Receptor/ERR
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Cancer
|
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-B1864C
-
|
Ksg sulfate
|
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
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-
- HY-P2138
-
|
|
HIV Protease
|
Others
|
|
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
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-
- HY-170523
-
|
|
SARS-CoV
DNA Methyltransferase
|
Infection
|
|
RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models .
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-
- HY-117839
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
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-
- HY-121490
-
|
|
Apoptosis
|
Cancer
|
|
IMM-02 is a DID-DAD binding inhibitor with activity promoting actin assembly and microtubule stabilization. IMM-02 is able to trigger serum response factor-mediated gene expression and lead to cell cycle arrest and apoptosis. IMM-02 has shown the ability to slow tumor growth in a mouse colon cancer xenograft model .
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-
- HY-170874
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
|
-
- HY-117649
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
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-
- HY-147736
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
|
-
- HY-147735
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 1 (compound 3e) is a potent GABAA receptor agonist. GABAA receptor agonist 1 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 1 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 1 has the potential for the research of depression .
|
-
- HY-W757743
-
|
ACP-196-d3
|
Isotope-Labeled Compounds
|
Others
|
|
Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
|
-
- HY-103552
-
|
|
mGluR
|
Neurological Disease
|
|
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
|
-
- HY-112863
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt inhibitor 3 is an orally active and potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor. RORγt inhibitor 3 shows high binding affinity and inhibitory activity of Th17 cell differentiation. RORγt inhibitor 3 also shows efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models .
|
-
- HY-145644
-
|
C-135-LS; BMS-986414
|
SARS-CoV
|
Infection
Cancer
|
|
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
|
-
- HY-171317
-
|
|
Bacterial
|
Infection
Neurological Disease
|
|
SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide (HY-B0276), enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models .
|
-
- HY-N0830S22
-
-
- HY-144705
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
|
-
- HY-129931
-
|
H-Phe-Phe-NH2
|
Neurokinin Receptor
|
Neurological Disease
|
|
Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) is a ligand for the substance P 1–7 (SP1-7) binding site with a Ki value of 1.5 nM. Phenylalanylphenylalanylamide exerts significant anti-allodynic and anti-hyperalgesic effects in animal models of neuropathic pain following central administratio. Phenylalanylphenylalanylamide shows no distinct effect after peripheral (intraperitoneal) administration. Phenylalanylphenylalanylamide can be used for research on pain-related diseases .
|
-
- HY-B0027R
-
|
|
Reference Standards
Antibiotic
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
|
Valnemulin (hydrochloride) (Standard) is the analytical standard of Valnemulin (hydrochloride). This product is intended for research and analytical applications. Valnemulin (hydrochloride) is an orally effective truncated pleurotin antibiotic that inhibits protein synthesis in bacteria by binding to peptidyl transferase in the 50s ribosome subunit. Valnemulin hydrochloride effectively eliminates Mycobacterium bovis in the lungs in an experimental bovine model of Mycoplasma bovis infection. Valnemulin hydrochloride can reduce the mortality of epidemic rabbit enteropathy and has no adverse effect on the growth performance of rabbits .
|
-
- HY-P991353
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
|
-
- HY-12168B
-
|
(Rac)-BAY 12-9566
|
MMP
|
Cancer
|
|
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models .
|
-
- HY-170586
-
-
- HY-173474
-
|
|
Estrogen Receptor/ERR
Androgen Receptor
|
Cancer
|
|
ERβ agonist-1 (Compound 8) is a dual-active selective ERβ agonist (EC50: 46.8 nM) and AR antagonist (IC50: 1555 nM). ERβ agonist-1 activates ERβ signaling by binding to ERβ and inhibits AR activity. ERβ agonist-1 retains selective ERβ agonist activity in mouse models and can be used to study prostate cancer .
|
-
- HY-B1864AR
-
|
Ksg hydrochloride (Standard)
|
Reference Standards
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride (Standard) is the analytical standard of Kasugamycin hydrochloride (HY-B1864A). This product is intended for research and analytical applications. Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
|
-
- HY-148479
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
Bixalomer is a phosphate binder. Bixalomer can improve hyperphosphatemia in chronic kidney disease (CKD) rat model. Bixalomer reduces plasma phosphorus level in CKD rat models through binding phosphate in small intestine and reduces phosphate absorption. Bixalomer can be studied in research on hyperphosphatemia .
|
-
- HY-181673
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma .
|
-
- HY-183314
-
|
|
Flavivirus
|
Infection
|
|
ZIKV-IN-9 is a ZIKV inhibitor that blocks the early binding of viral particles to the cell surface. ZIKV-IN-9 inhibits ZIKV in various cell models. ZIKV-IN-9 is applicable to research related to Zika virus infection .
|
-
- HY-183354
-
|
|
Histone Methyltransferase
WDR5
Apoptosis
Caspase
|
Cancer
|
|
HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model .
|
-
- HY-180800
-
|
|
COX
|
Neurological Disease
Inflammation/Immunology
|
Anti-inflammatory agent 110 (Compound 7b) is a analgesic/anti-inflammatory agent. Anti-inflammatory agent 110 has a good binding affinity for COX-2. Anti-inflammatory agent 110 demonstrated potent analgesic and anti-inflammatory activities in the mouse hot plate test and the rat carrageenan edema model .
|
-
- HY-120031
-
|
|
STAT
PARP
Apoptosis
|
Cancer
|
|
NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer .
|
-
- HY-W142795
-
|
4-sec-BP
|
Androgen Receptor
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
4-sec-Butylphenol (4-sec-BP) is an androgen receptor ligand that binds to the androgen receptor with a pIC50 of 4.07 . 4-sec-Butylphenol is an estrogen receptor agonist. 4-sec-Butylphenol can be found in industrial effluents, in production water of oil and gas platforms, as well as in river water samples .
|
-
- HY-P11618
-
|
|
Glycoprotein VI
|
Cancer
|
|
10P3Me is a Glypican-3 (GPC3)-targeting probe with a Ka of 93.8 nM for the human target. 10P3Me exhibits high binding affinity to GPC3, targets GPC3-positive cells, and serves as an agent for PET imaging. 10P3Me selectively accumulates in GPC3-positive tumor tissues, including subcutaneous xenograft models and orthotopic HepG2-LUC liver cancer models, to achieve precise localization of lesions .
|
-
- HY-12435
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis .
|
-
- HY-157828
-
|
|
Emopamil Binding Protein
|
Neurological Disease
Cancer
|
|
DSP-0390 is an orally effective inhibitor of Emopamil-binding protein (EBP). DSP-0390 blocks the cholesterol de novo synthesis pathway in tumor cells by inhibiting EBP, and demonstrates significant anti-tumor activity in an orthotopic xenograft model of glioblastoma (GBM). DSP-0390 can be used for the study of recurrent high-grade gliomas .
|
-
- HY-P992474
-
|
|
Interleukin Related
STAT
CCR
Fc Receptor (FcR)
|
Inflammation/Immunology
|
|
TAVO101 is a humanized anti-TSLP antibody with an EC50 of 0.19 nM against hTSLP. TAVO101 inhibits STAT5 activation and CCL17 release. TAVO101 carries Fc region mutations that enhance its binding to FcRn while reducing its binding to FcγRI, FcγRIIIA and C1q, thereby attenuating effector functions. TAVO101 reduces the levels of inflammatory markers, cell infiltration and histopathological damage in preclinical models of asthma, psoriasis and atopic dermatitis. TAVO101 can be used for research related to asthma, psoriasis and atopic dermatitis .
|
-
- HY-103423R
-
|
|
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
PAOPA (Standard) is the analytical standard of PAOPA (HY-103423). This product is intended for research and analytical applications. PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists .
|
-
- HY-N17727
-
|
|
Interleukin Related
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Divaricatol is an orally ative chromone natural product and an active component in Saposhnikovia divaricata. Divaricatol reduces the release of pro-inflammatory cytokines and restores immune homeostasis by stably binding to 5KIR (a target of the TNF/IL-17 pathway). Divaricatol exerts analgesic effects in mouse models. Divaricatol can be used in the research of pain, diarrhea-predominant irritable bowel syndrome (IBS-D) and qi deficiency syndrome .
|
-
- HY-18314B
-
|
|
Orphan Nuclear Receptor
Ferroptosis
|
Cardiovascular Disease
|
|
(Z)-GW 441756 is a hepatocyte nuclear factor 4α (HNF4α) activator, with an EC50 of 9.2 μM and a Ka of 4.6 μM in human systems. (Z)-GW 441756 directly interacts with the ligand-binding domain of HNF4α via persistent hydrogen bonds and hydrophobic interactions within the binding pocket. (Z)-GW 441756 reduces the accumulation of triglycerides and total cholesterol. (Z)-GW 441756 inhibits ferroptosis through a non-antioxidant mechanism. (Z)-GW 441756 decreases plasma triglyceride and total cholesterol levels in animal models of hyperlipidemia. (Z)-GW 441756 can be used in studies related to hyperlipidemia .
|
-
- HY-D3192
-
|
|
Fluorescent Dye
Bacterial
Amyloid-β
|
Infection
|
|
CDy11 is a fluorescent probe and amyloid-binding dye (λex=590 nm; λem=612 nm), with a Ka of 29 μM for Pseudomonas aeruginosa Fap. CDy11 specifically recognizes amyloid fibrils in bacterial biofilms and exhibits significantly enhanced fluorescence upon binding to the target. CDy11 shows no staining effect on amyloid-deficient mutant strains, planktonic cells or protein monomers. CDy11 supports in vivo imaging of Pseudomonas aeruginosa biofilms in mouse implant and corneal infection models. CDy11 is widely used in studies of Staphylococcus aureus biofilm infections, dental caries, and Pseudomonas aeruginosa-associated implant and corneal infections .
|
-
- 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-19220
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
S-18326 is an orally active direct thrombin inhibitor. S-18326 inhibits thrombus formation by reversibly and with high affinity binding to the active site of thrombin, directly preventing the conversion of fibrinogen to fibrin. S-18326 effectively prolongs various clotting times in human plasma. S-18326 has demonstrated antithrombotic efficacy in multiple animal models without causing thrombocytopenia. S-18326 can be used in research on thromboembolic diseases .
|
-
- HY-157214
-
|
|
STING
Molecular Glues
|
Cancer
|
|
NVS-STG2 is a molecular glue that targets STINGbinding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- 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-173016
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-160998
-
|
|
CCR
|
Inflammation/Immunology
|
|
YM-344031 is an orally active antagonist for CCR3. YM-344031 inhibits binding of Eotaxin-1 and RANTES to CCR3, with IC50 of 3.0 and 16.3 nM. YM-344031 inhibits ligand-induced rise in intracellular Ca [2+] and the ligand-induced chemotaxis. YM-344031 inhibits eotaxin-1-induced changes in eosinophil morphology in macaques blood, and prevents allergic skin reactions in a mouse allergy model .
|
-
- HY-P992473
-
|
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
TAS266 is a tetrameric nanobody agonist targeting DR5. TAS266 selectively induces cancer cell death. TAS266 triggers sustained tumor regression in xenograft models and also elicits immunogenic responses including antibody binding. TAS266 exhibits superior anti-tumor efficacy compared with traditional DR5-targeting strategies. TAS266 can be used in research related to pancreatic cancer and advanced solid tumors .
|
-
- HY-118156
-
|
|
Others
|
Others
|
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
- HY-P992342
-
|
|
Tim3
|
Cancer
|
|
DCB-8 is a specific inhibitor targeting human TIM-3. DCB-8 regulates T cell function, enhances cytokine secretion, and inhibits tumor growth in disease animal models. DCB-8 can be used for cancer research .
|
-
- HY-180473
-
-
- HY-165559
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC50s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology .
|
-
- HY-153898
-
|
|
Amyloid-β
|
Neurological Disease
|
|
rTRD01 is an orally active, specific TDP-43 binder that targets the RRM1 and RRM2 domains of TDP-43. rTRD01 partially disrupts the interaction between TDP-43 and c9orf72 repeat RNA, but does not affect the binding of TDP-43 to canonical binding sequences. rTRD01 exhibits significant neuroprotective effects in zebrafish models, improves motor function and protects against paraquat (a widely used herbicide)-induced neurodegeneration, with no teratogenicity at high concentrations. rTRD01 is not a general antioxidant and cannot counteract Rotenone (HY-B1756)-induced neuronal death. rTRD01 can be used to study amyotrophic lateral sclerosis and other TDP-43 proteinopathies .
|
-
- HY-181675
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma .
|
-
- HY-12193
-
|
|
Histamine Receptor
|
Others
|
|
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
|
-
- HY-181020
-
|
|
Phosphodiesterase (PDE)
p38 MAPK
Akt
mTOR
ERK
|
Cancer
|
|
Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma .
|
-
- HY-160921
-
|
SL65.0155 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .
|
-
- HY-122611R
-
|
|
Reference Standards
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-17600A
-
|
Calquence maleate; ACP-196 maleate
|
Btk
|
Cancer
|
|
Acalabrutinib (Calquence) maleate is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib maleate demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib maleate can be used for CLL research . Acalabrutinib maleate is a click chemistry reagent, which contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N1486R
-
|
3-Ketoursolic acid (Standard)
|
Reference Standards
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- 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 .
|
-
- HY-17600
-
|
Calquence; ACP-196
|
Btk
|
Inflammation/Immunology
Cancer
|
|
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib can be used for CLL research . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P1220
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P1220A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-B1864BR
-
|
Ksg hydrochloride hydrate (Standard)
|
Reference Standards
Antibiotic
Bacterial
|
Infection
|
|
Kasugamycin (Ksg) hydrochloride hydrate (Standard) is the analytical standard of Kasugamycin hydrochloride hydrate (HY-B1864B). This product is intended for research and analytical applications. Kasugamycin (Ksg) hydrochloride hydrate is an antibiotic that binds to 30s and 70s ribosomes but not to the 50s subunit, and has anti-infective activity. Kasugamycin hydrochloride hydrate mimics mRNA nucleotides, disrupts tRNA binding and inhibits canonical translation initiation. Kasugamycin hydrochloride hydrate increases the sensitivity of mycobacteria to Rifampicin (HY-B0272) in vitro and in mouse infection models .
|
-
- HY-144256
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
CHD1Li 6.11 is a potent and orally active Chromodomain Helicase DNA Binding Protein 1 Like (CHD1L) (oncogenic gene) inhibitor (IC50 = 3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 can inhibit EMT, induce mesenchymal-epithelial transition (reverse EMT) and promote apoptosis in tumor organoid models. CHD1Li 6.11 can be used for the research of cancer, such as colorectal cancer .
|
-
- 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-182404
-
|
|
Free Fatty Acid Receptor
|
Cancer
|
|
Anticancer agent 316 (Compound 1) is an anticancer agent. Anticancer agent 316 exerts anticancer activity against colorectal cancers expressing GPR120. Anticancer agent 316 can be used in the research of colorectal cancer .
|
-
- HY-107830R
-
|
|
Reference Standards
Endogenous Metabolite
Collagen
|
Metabolic Disease
|
|
Methyl cholate (Standard) is the analytical standard of Methyl cholate. This product is intended for research and analytical applications. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
|
-
- HY-159098
-
|
|
Molecular Glues
PROTACs
Histone Acetyltransferase
|
Cardiovascular Disease
|
|
dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
|
-
- HY-W746556
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Collagen
|
Metabolic Disease
|
|
Methyl cholate-d5 is the deuterium labeled Methyl cholate. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
|
-
- HY-182037
-
|
|
DNA/RNA Synthesis
Pyruvate Kinase
|
Cancer
|
|
Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research .
|
-
- 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 .
|
-
- HY-124693
-
|
|
Apoptosis
|
Cancer
|
|
DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34+ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia[1].
|
-
- HY-159585
-
|
|
Cytochrome P450
Fungal
|
Infection
|
|
CYP51-IN-20 (compound 5b) is an inhibitor of CYP51 and has antifungal activity. CYP51-IN-20 has a significant inhibitory effect on Candida albicans ATCC 10231, downregulates ERG11 (Cyp51) gene expression, and significantly reduces the yeast-to-hyphae morphological transition. CYP51-IN-20 can synergize with Voriconazole (HY-76200) to occupy the entire CYP51 binding site and exert a synergistic inhibitory effect in the Glechoma moth model .
|
-
- HY-118424
-
|
|
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 .
|
-
- HY-17600R
-
|
ACP-196 (Standard)
|
Reference Standards
Btk
|
Cancer
|
|
Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-174270
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
NEKs
|
Inflammation/Immunology
|
|
NLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis .
|
-
- 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 .
|
-
- HY-182936
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Antibacterial agent 338 (Compound 65) is an antibacterial agent and GyrB inhibitor, with an IC50 of 12.60 nM against GyrB from E. coli. Antibacterial agent 338 binds to the ATP-binding domain of E. coli GyrB, thereby inhibiting the ATPase activity of GyrB. Antibacterial agent 338 exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria. Antibacterial agent 338 reduces bacterial load in a neutropenic mouse thigh infection model. Antibacterial agent 338 can be used for the research of Acinetobacter baumannii infection .
|
-
- HY-P2460
-
|
|
Bacterial
Fungal
Interleukin Related
TNF Receptor
|
Infection
Inflammation/Immunology
|
|
SMAP‑29 is a cathelicidin antimicrobial peptide with LPS‑binding and anti‑inflammatory properties. SMAP‑29 exerts broad‑spectrum antimicrobial activity against bacteria, fungi and multidrug‑resistant isolates. SMAP‑29 kills pathogens by permeabilizing bacterial membranes, inducing depolarization and cell lysis, and also inhibits inflammatory cytokines while reducing lethality in septic shock and pneumonia models. SMAP-29 can be used for research on bacterial infections, drug-resistant infections, septic shock .
|
-
- HY-156815
-
|
|
Orphan GPCR
|
Neurological Disease
Inflammation/Immunology
|
|
YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain .
|
-
- HY-124388
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-20 is a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor with anti-TNF-α properties. PDE4-IN-20 exhibits significant biological activity in vitro and in vivo. The mechanism of action of PDE4-IN-20 is supported by molecular modeling studies, which reveal its binding mode with PDE4. PDE4-IN-20 was optimized in further conformational analysis and showed pharmacological characteristics similar to those of known PDE4 inhibitors .
|
-
- HY-12927
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-168948
-
|
|
Bacterial
|
Infection
|
|
Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding PqsR proteins. Quorum sensing-IN-9 inhibits the expression of quorum sensing systems related genes lasB, rhlA and pqsA, blocks the generation of virulence factors elastase, pyocyanin and rhamnolipid. Quorum sensing-IN-9 destorys the motility of P. aeruginosa, inhibits the biofilm formation, decreasing the virulence and pathogenicity of P. aeruginosa. Quorum sensing-IN-9 exhibits anti-infectious activity in Galleria mellonella larval model .
|
-
- 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-176758
-
|
|
Glutathione Peroxidase
|
Cancer
|
|
GPX4-IN-17 (Compound 9i) is an inhibitor of GPX4 with potent cytotoxicity (IC50 = 0.3 nM). GPX4-IN-17 shows strong binding affinity against GPX4 (KD = 20.4 nM). GPX4-IN-17 inhibits tumor growth in the xenograft tumor mouse model without detectable cytotoxicity. GPX4-IN-17 can enhance cancer chemotherapy and overcome tumor resistance. GPX4-IN-17 can be studied in antitumor reseach .
|
-
- HY-P992066
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
|
|
Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis .
|
-
- HY-170925
-
|
|
Cholinesterase (ChE)
Apoptosis
|
Neurological Disease
|
|
AChE-IN-81 (compound 22) is a potent, irreversible and selective AChE inhibitor. AChE-IN-81 inhibits activity on AChE with inhibitory rates of 80.0%, with an IC50 of 3.7 μM. AChE-IN-81 binds to AChE with a binding affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces in zebrafish brain cells. AChE-IN-81 exhibits potential neuroprotective activities on H2O2-induced SH-SY5Y cell injury model .
|
-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
Cancer
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
|
-
- HY-N11768
-
|
|
NF-κB
Interleukin Related
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .
|
-
- HY-19487
-
|
|
Bacterial
|
Infection
|
|
Ribocil is a selective inhibitor targeting the bacterial FMN riboswitch, regulating the bacterial riboflavin riboswitch. Ribocil competitively binds to the FMN binding site, mimicking the natural ligand FMN to induce conformational changes in the riboswitch, inhibiting ribB gene expression, reducing riboflavin synthesis, and thus inhibiting bacterial growth. Ribocil strongly inhibits GFP expression (EC50=0.3 μM). Ribocil exhibits in vivo antibacterial activity in a mouse model and can be used to study antibacterial drugs related to drug-resistant bacterial infections and bacterial riboflavin metabolic pathways[1][2].
|
-
- HY-P991447
-
|
|
VISTA
|
Cancer
|
|
Anti-VSIR/VISTA Antibody (SG7) is a human monoclonal antibody (mAb) targeting VISTA/B7-H5. Anti-VSIR/VISTA Antibody (SG7) inhibits VISTA function and prevents PSGL-1 and VSIG3 from binding to VISTA. Anti-VSIR/VISTA Antibody (SG7) has anti-tumor activity in the mouse B16F10 melanoma model. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-176537
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
|
-
- HY-179459
-
|
|
Wnt
LDLR
Amyloid-β
|
Neurological Disease
|
|
SJ-300 is a potent and selective, orally active and brain-penetrat DKK3-LRP1 interaction inhibitor. SJ-300 restores Aβ clearance in AD models. SJ 300 binds to mLRPIV with a Kd of 7.9 μM, inhibits the DKK3 mLRPIV complex with an IC50 of 3.2 μM, and does not disrupt the binding of Aβ to LRP1. SJ 300 rescues cognitive function and ameliorates neuropathology (Aβ plaque reduction ≈ 73.3 %) in vivo. SJ 300 can be employed for research in Alzheimer’s disease .
|
-
- 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-155356
-
|
|
PROTACs
Ras
|
Cancer
|
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
|
-
- HY-179371
-
|
|
Pyruvate Kinase
Interleukin Related
|
Inflammation/Immunology
|
|
LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC50 = 0.39 μM; Kd = 4.5 μM) targeting Arg43 within the polyarginine pocket. LIQ1 exhibits efficacy in a mouse model of LPS (HY-D1056)-induced endotoxemia, preventing the nuclear translocation of PKM2 and inhibiting its binding to HIF-1α, thereby suppressing IL-1β transcription. LIQ1 can be used for the research of endotoxemia [1].
|
-
- 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]
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- HY-178342
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Xanthine Oxidase
Reactive Oxygen Species (ROS)
SOD
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Metabolic Disease
Inflammation/Immunology
Cancer
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Xanthine oxidase-IN-18 is a potent orally activeXanthine oxidase (XO) inhibitor (IC50 = 0.263 μM). Xanthine oxidase-IN-18 exerts inhibition by directly and stably binding to the xanthine oxidase Mo-co active site. Xanthine oxidase-IN-18 exhibits reactive oxygen species (ROS) scavenging activity. Xanthine oxidase-IN-18 shows anti-hyperuricemia effects in a Potassium oxonate (HY-17511)-induced hyperuricemic rat model. Xanthine oxidase-IN-18 can be used for hyperuricemia, breast and lung cancer research .
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- HY-122179
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TGF-β Receptor
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Inflammation/Immunology
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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-112974
-
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GSK-2998728; ISIS-420915
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Transthyretin (TTR)
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Cardiovascular Disease
Neurological Disease
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Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy .
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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-33299
-
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BTCA
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Biochemical Assay Reagents
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Cancer
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Serpin B9-IN-1 (BTCA) is an inhibitor that specifically targets Serpin B9 (SB9); SB9 is a natural inhibitor of granzyme B (GrB) , but may promote the metastasis of lung cancer cells into the bone marrow. SB9-overexpressing cancer cells promote proliferation and metastasis in an immune cell-dependent manner by binding to GrB. Inhibition of SB9 by Serpin B9-IN-1 significantly inhibits immunotherapy of lung cancer bone metastases in the caudal artery (CA) mouse model (LCBM) .
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- HY-163410
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PROTACs
Epigenetic Reader Domain
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Cancer
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AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)) .
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- HY-P991598
-
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MOR12743; MOR03207
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Interleukin Related
NF-κB
|
Inflammation/Immunology
|
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MOR-106 (MOR12743) is a humanized anti-IL-17C IgG1 monoclonal antibody. MOR-106 inhibits the NF-κB signaling pathway by specifically binding to IL-17C (IC50 = 59 pM for human IL-17C, IC50 = 55 pM for mouse IL-17C). MOR-106 can effectively inhibit skin inflammation and reduce related inflammatory factors in animal models of psoriasis and atopic dermatitis .
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- HY-107588
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TC-I 15
2 Publications Verification
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Integrin
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Cardiovascular Disease
|
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TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
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- HY-160822
-
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PF-5212371
|
ADAMTS
MMP
|
Inflammation/Immunology
|
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AGG-523 (PF-5212371) is an orally active, reversible, non-hydroxamate, zinc-binding selective inhibitor of ADAMTS4 and ADAMTS5 with IC50 of <0.03 and 0.04 μM. AGG-523 also inhibits MMP-2, -8, 12 activity AGG-523 attenuates release of aggrecanase-generated ARG-aggrecan fragments into synovial fluid, reduces surgery-induced ARG-aggrecan release in rat joint models, and inhibits aggrecanase activity to slow cartilage degradation. AGG-523 can be used for the research of osteoarthritis .
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- HY-19210
-
|
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Endothelin Receptor
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Cardiovascular Disease
|
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SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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- HY-P990004
-
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Tim3
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Inflammation/Immunology
Cancer
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Anti-Mouse TIM-3 Antibody (B8.2C12) is an anti-mouse TIM-3 IgG1 monoclonal antibody. Anti-Mouse TIM-3 Antibody (B8.2C12) can block the binding of Tim-3 with Phosphatidylserine (PtdSer) and CEACAM1 without interfering with the binding to Galectin-9. Anti-Mouse TIM-3 Antibody (B8.2C12) can inhibit tumor growth and activate tumor infiltrating CD8 + T cells. Anti-Mouse TIM-3 Antibody (B8.2C12) can be used for studying cancer such as breast cancer and colon cancer and constructing experimental autoimmune encephalomyelitis (EAE) models .
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- HY-159520
-
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Ofirnoflast; HT-6184
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NEKs
NOD-like Receptor (NLR)
Caspase
Apoptosis
Pyroptosis
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
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Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
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- HY-W015050
-
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1-Aminoanthracene
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GABA Receptor
Chloride Channel
Fluorescent Dye
|
Neurological Disease
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1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with Kd = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC50 value of 16 μM .
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- HY-182895
-
|
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Influenza Virus
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Infection
|
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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-P992082
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VEGFR
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Cancer
|
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Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF . The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
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- HY-180159
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin-IN-63 is a potent tubulin polymerization inhibitor targeting the colchicine-binding site, with an IC50 of 6.03 µM. Tubulin-IN-63 disrupts microtubule dynamics, induces G2/M arrest and apoptosis, thereby suppressing cancer cell proliferation. Tubulin-IN-63 disrupts capillary network formation in human umbilical vein endothelial cells (HUVECs) and exhibits in vivo antitumor efficacy in a B16-F10 mouse model. Tubulin-IN-63 can be used for the research of cancers, such as melanoma, lung cancer, and liver cancer .
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- HY-P992388
-
|
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LILRB
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Cancer
|
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IO-108 is a humanized IgG4 monoclonal antibody and a competitive inhibitor of LILRB2, with a KD value of 1.97 nM. IO-108 competitively blocks the binding of LILRB2 to its ligands including HLA-G, MHC-I, ANGPTL2 and SEMA4A, reprograms tumor-associated myeloid cells, drives the conversion of suppressive myeloid cells into a pro-inflammatory phenotype, and restores the cytotoxic activity of T cells and NK cells. IO-108 inhibits tumor growth in LILRB2 transgenic mouse models. IO-108 can be used for the research of solid tumors .
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- HY-129085
-
|
C5OH
|
Drug Derivative
Apoptosis
NF-κB
|
Cancer
|
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5-Methyl cromolyn (C5OH) disodium, an analog of Cromolyn (HY-B1619), is a S100P inhibitor. 5-Methyl cromolyn disodium inhibits the binding of S100P to its receptor RAGE, NF-κB activity and cell proliferation, and promotes Gemcitabine (HY-17026)-induced apoptosis. 5-Methyl cromolyn disodium reduces tumor growth and metastasis, and prolongs survival in mouse models of syngeneic PDAC. 5-Methyl cromolyn disodium can be used for pancreatic cancer like pancreatic ductal adenocarcinoma (PDAC) research .
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- HY-100555
-
|
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HSP
|
Infection
Cancer
|
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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 .
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- HY-182367
-
|
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GPR39
|
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-P10870
-
|
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Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
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Cancer
|
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Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
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- HY-P991270
-
|
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Interleukin Related
|
Inflammation/Immunology
|
|
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
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- HY-W181530
-
|
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Molecular Glues
CDK
Apoptosis
Ligands for E3 Ligase
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Cancer
|
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NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
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- HY-123960
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Raphin1
3 Publications Verification
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Phosphatase
|
Neurological Disease
|
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Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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- HY-123960A
-
|
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Phosphatase
|
Neurological Disease
|
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Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
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- HY-186087
-
|
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Ras
ERK
Cyclophilin
|
Cancer
|
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RM-046 is an orally active, selective ternary complex inhibitor of KRAS Q61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRAS Q61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRAS Q61H mutant cancers .
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- HY-117380
-
|
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Neurokinin Receptor
|
Neurological Disease
|
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SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .
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- HY-103490
-
|
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
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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 .
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- HY-181652
-
|
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PPAR
|
Endocrinology
|
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PPARδ agonist 13 is a potent, selective and orally active PPARδ agonist with an EC50 values of 0.50 nM. PPARδ agonist 13 binds to the PPARδ ligand-binding pocket and upregulates PPARδ target gene expression. PPARδ agonist 13 inhibits renal fibroblast activation, restores fatty acid oxidation, and attenuates TGF-β1-induced renal fibroblast activation. PPARδ agonist 13 exhibits anti-renal fibrosis effects in a mouse model of unilateral ureteral obstruction. PPARδ agonist 13 can be used for the research of renal fibrosis .
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- HY-P991584
-
|
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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 .
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- HY-182039
-
|
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Microtubule/Tubulin
Caspase
Apoptosis
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Cancer
|
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Tubulin polymerization-IN-89 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-89 binds to the colchicine-binding site on tubulin heterodimers, disrupting tubulin polymerization and microtubule formation. Tubulin polymerization-IN-89 induces apoptosis in melanoma cells and arrests the cell cycle at the G2/M phase. Tubulin polymerization-IN-89 can be used in studies related to metastatic melanoma .
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- HY-164992
-
|
MRG002; Trastuzumab MMAE
|
Antibody-Drug Conjugates (ADCs)
EGFR
Microtubule/Tubulin
|
Cancer
|
|
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
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- HY-P992062
-
|
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PD-1/PD-L1
|
Inflammation/Immunology
|
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Anti-Mouse CD80 Antibody (TKMG48) is an antibody that targets mouse CD80. By specifically binding to and disrupting the CD80:PD-L1 complex to release PD-L1, Anti-Mouse CD80 Antibody (TKMG48) functions as an indirect PD-1 agonist without blocking CD28 co-stimulation or CD80-CTLA4 binding. Anti-Mouse CD80 Antibody (TKMG48) inhibits T cell activation, reduces T cell effector functions and antigen-specific CD8 + T cell populations, and does not interfere with the differentiation, migration, antigen presentation or surface marker expression of dendritic cells. Anti-Mouse CD80 Antibody (TKMG48) significantly attenuates disease severity in mouse models of arthritis, spondyloarthritis, multiple sclerosis and Sjögren's syndrome, and its activity depends on the expression of PD-1 and PD-L1 .
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- HY-110333
-
|
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EGFR
|
Cancer
|
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BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
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- HY-179505
-
|
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YAP
|
Cancer
|
|
OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research .
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- HY-P990673
-
|
DSTP-3086S Antibody; RG-7450 Antibody
|
ADC Antibody
Transmembrane Glycoprotein
Mitosis
|
Cancer
|
|
Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
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- HY-116142
-
|
|
iGluR
|
Neurological Disease
|
|
CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
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-
- HY-W195984
-
|
|
Phosphoglycerate Kinase (PGK)
|
Cancer
|
|
Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer .
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-
- HY-182764A
-
|
|
CDK
|
Cancer
|
|
CDK11-IN-1 hydrochloride is a potent, highly selective, and orally active CDK11 inhibitor with an IC50 of 4 nM, showing 32.5-fold and 2700-fold selectivity over CDK7 and CDK9, respectively. CDK11-IN-1 hydrochloride binds competitively to the ATP-binding pocket of CDK11 and forms a hydrogen bond with the hinge region residue Val163. It inhibits tumor cell proliferation and exhibits antitumor activity in lung cancer xenograft models. CDK11-IN-1 hydrochloride can be used for studies on the pathophysiology of CDK11-mediated tumors, as well as research on malignant tumors such as lung cancer .
|
-
- HY-181778
-
|
|
SARS-CoV
DNA/RNA Synthesis
|
Infection
|
|
RdRP-IN-10 is a SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor with an IC50 value of 5.78 μM. RdRP-IN-10 forms covalent binds with SARS-CoV-2 nsp8 Cys114, disrupts nsp8-nsp12 stabilizing interactions. RdRP-IN-10 inhibits SARS-CoV-2 RdRp-mediated RNA polymerization without interfering with RNA-RdRp complex binding. RdRP-IN-10 exerts antiviral effects in cellular models. RdRP-IN-10 can be used for the research of SARS-CoV-2 infection .
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-
- HY-147081
-
AS 1411
2 Publications Verification
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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-
- HY-P990778
-
|
ATG-101
|
TNF Receptor
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Xirestomig (ATG-101) is a tetravalent "2+2″ PD-L1×4-1BB bispecific antibody. Xirestomig binds PD-L1 and 4-1BB concurrently, with a greater affinity for PD-L1, and potently activated 4-1BB+ T cells when cross-linked with PD-L1-positive cells. Xirestomig activates exhausted T cells upon PD-L1 binding. Xirestomig displays potent antitumor activity in numerous in vivo tumor models, including those resistant or refractory to immune checkpoint inhibitors (ICIs) .
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-
- 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 .
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-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
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Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
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- HY-P10786
-
|
|
Transmembrane Glycoprotein
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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 .
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- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
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Cancer
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|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
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- HY-B1824
-
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HR-810 sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Cefpirome (HR-810) sulfate is a cephalosporin antibiotic that can cross cell membranes and the blood-brain barrier. Cefpirome sulfate binds to penicillin-binding proteins with high affinity, thereby inhibiting bacterial cell wall synthesis. Cefpirome sulfate exhibits bactericidal and growth-inhibitory activities against Gram-negative bacteria, Gram-positive bacteria, and susceptible anaerobic bacteria (including some β-lactamase-producing strains) .
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- HY-175698
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ACSL Family
Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
|
Cancer
|
|
Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [ 3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC) .
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-
- HY-100685
-
MS-444
2 Publications Verification
BE-34776
|
HuR
Apoptosis
COX
|
Neurological Disease
Cancer
|
|
MS-444 (BE-34776) is a HuR (ELAVL1) inhibitor that blocks the cytoplasmic translocation of HuR and inhibits its dimerization. MS-444 reduces cytoplasmic HuR levels by preventing the binding of HuR to ARE-mRNA, without altering the total expression of HuR. MS-444 induces apoptosis, inhibits cell growth, angiogenesis and invasion, and also regulates immune function and microbiota. MS-444 effectively alters the number, size and invasiveness of tumors in various cancer models. MS-444 is tolerable to intraperitoneal injection in vivo and can be applied to research related to colorectal cancer, familial adenomatous polyposis, colitis-associated cancer and glioblastoma .
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- HY-180557
-
|
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Folate Receptor (FR)
|
Cancer
|
|
4A-BFA-11 is a folate-targeted PEG-MMAE conjugate that exhibits specific binding affinity for the folate receptor α (FR-α) (KD = 106.7 nM). 4A-BFA-11 achieves tumor enrichment by combining PEG-mediated long circulation (EPR effect) and folate receptor targeting. 4A-BFA-11 undergoes enzymatic cleavage at the tumor site to release the active payload, enabling precise action. 4A-BFA-11 sefficiently carries, targets, and controls the release of MMAE in tumor tissues in a HeLa mouse model. 4A-BFA-11 can be used for cervical cancer, ovarian cancer, and lung cancer research .
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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-182700
-
|
|
Complement System
VEGFR
|
Cancer
|
|
NRPa-308 is a potent and orally active Neuropilin-1 (NRP-1) antagonist with an IC50 of 42 μM for inhibiting VEGF-A165 binding to NRP-1. NRPa-308 blocks the specific interaction between VEGF-A165 and NRP-1. NRPa-308 effectively suppresses angiogenesis in vitro and in vivo and reduces the viability of a broad spectrum of human solid and haematological cancer cells. NRPa-308 inhibits tumor growth and prolongs median survival in a human breast cancer xenograft mouse model. NRPa-308 can be used for the research of multiple human malignancies including solid tumors and hematological cancers .
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-
- HY-145928
-
|
GDC-6036
|
Ras
|
Cancer
|
|
Divarasib (GDC-6036) is an orally active, selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRAS G12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRAS G12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRAS G12C-mutated solid tumors .
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-
- HY-147081A
-
|
AGRO-100 sodium
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
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-
- HY-182603
-
|
|
Drug Derivative
Reactive Oxygen Species (ROS)
HCV
|
Infection
Inflammation/Immunology
|
|
BO-653 is an orally active anti-atherosclerotic antioxidant that exhibits high binding affinity for LDL. BO-653 scavenges linoleic acid peroxyl radicals, inhibits lipid peroxidation during the auto-oxidation of linoleic acid, and potently suppresses LDL oxidation. BO-653 inhibits Hepatitis C Virus (HCV) replication in a concentration-dependent manner, with an IC50 of 36.0 μM against the HCV subgenomic replicon in FLR3-1 cells. BO-653 demonstrates significant anti-atherosclerotic effects in various animal models, including the Watanabe heritable hyperlipidemic rabbit. BO-653 is suitable for use in research related to atherosclerosis and Hepatitis C Virus infection .
|
-
- HY-179457
-
|
|
PI3K
mTOR
Akt
HSP
|
Cancer
|
|
CC-11 is an orally active small molecule drug conjugate (SMDC) that links the PI3K/mTOR inhibitor with the extracellular heat shock protein 90 (EHSP90) targeting ligand through a cleavable linker. CC-11 exhibits strong HSP90 binding activity (IC50 = 15 nM) and inhibits PI3Kα kinase activity (IC50 = 0.54 nM). CC-11 has anti-proliferative activity against colon cancer cells. CC-11 shows significant efficacy in the HCT-116 xenograft tumor model. CC-11 can be used for research on colon cancer .
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-
- HY-145928B
-
|
GDC-6036 adipate
|
Ras
|
Cancer
|
|
Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors .
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-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as Alzheimer's disease .
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-
- HY-P10861A
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease .
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-
- 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 .
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-
- HY-148907
-
|
|
CaMK
MEK
Mixed Lineage Kinase
RIP kinase
Tau Protein
|
Neurological Disease
|
|
CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC50 values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease .
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-
- HY-P992449
-
|
PRLR ADC antibody
|
ADC Antibody
|
Cancer
|
|
REGN2878 (PRLR ADC antibody) is a monoclonal antibody targeting the prolactin receptor (PRLR) and can block prolactin‑mediated activation of PRLR. REGN2878 exhibits an equilibrium dissociation constant (KD) of 1.05 nM and an IC50 of 0.344 nM for human PRLR. REGN2878 can be rapidly internalized and degraded in lysosomes by PRLR‑positive tumor cells, showing antigen‑specific binding and targeted enrichment properties. REGN2878 derivatives can be used as an immunoPET agent for antigen‑specific imaging of PRLR‑related tumors, and can also serve as a component of ADCs to exert anti‑tumor activity in breast cancer xenograft models. REGN2878 can be used in the research of breast cancer and prostate cancer. Isotype Comparison HY-P99001 .
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-
- HY-178343
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
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-
- HY-178166
-
|
|
Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research .
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-
- HY-173182
-
|
|
Microtubule/Tubulin
P-glycoprotein
|
Cancer
|
|
Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field .
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-
- HY-172113
-
|
|
PROTACs
YAP
c-Myc
Apoptosis
|
Cancer
|
|
H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma .
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-
- HY-W663179
-
|
|
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 .
|
-
- HY-181529
-
|
|
VDAC
PERK
|
Cancer
|
|
NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2 and VDAC3. NCATS-SM0225 exhibits an IC50of 1.02 μM for ERAD and a Kd of 3.13 μM for human VDAC1 binding. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling and activating PERK. NCATS-SM0225 selectively kills cancer cells, exhibits tumor growth inhibitory effects in melanoma xenograft models. NCATS-SM0225 can be used for research on multiple cancers including melanoma, as well as the molecular mechanisms of ERAD and calcium homeostasis regulation .
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-
- HY-182068
-
|
|
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
NFI23 is a GluN2B-NMDAR inhibitor with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 can cross the blood-brain barrier. NFI23 binds to the ifenprodil binding site of GluN2B-NMDAR, reduces NMDA-induced Ca 2+ influx and reactive oxygen species (ROS) production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke .
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-
- HY-W140439
-
|
18:1 Lyso PC
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
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-
- HY-107588R
-
|
|
Reference Standards
Integrin
|
Cardiovascular Disease
|
|
TC-I 15 (Standard) is the analytical standard of TC-I 15 (HY-107588). This product is intended for research and analytical applications. TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
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-
- HY-178169
-
|
|
Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research .
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-
- HY-175455
-
|
|
PROTACs
Androgen Receptor
Akt
|
Cancer
|
|
LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC). (Pink: AR-DBD ligand-1: HY-175456, Blue: Thalidomide: HY-14658, Pink + Black: AR-DBD ligand-Linker Conjugate 1: HY-175457, Black: Boc-piperidine-oxopiperidin: HY-175458) .
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-
- HY-182372
-
|
|
Epoxide Hydrolase
|
Neurological Disease
|
|
SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
|
-
- HY-101741
-
|
A-289099
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
|
-
- HY-103490R
-
|
EDHS-206 (Standard)
|
Reference Standards
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (Standard) is the analytical standard of Takinib. This product is intended for research and analytical applications. Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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-
- HY-B2004
-
|
|
Environmental Pollutants
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Thifluzamide is a fungicide that inhibits fungal respiration by blocking the ubiquinone-binding site in mitochondrial complex II. Thifluzamide exhibits significant activity against Basidiomycota pathogens (such as Rhizoctonia cerealis, Ustilago and Puccinia genera) and is commonly used in studies on wheat sharp eyespot. Thifluzamide displays a dual mechanism in regulating lipid metabolism: it reduces fatty acid synthase activity to inhibit endogenous fatty acid synthesis, and increases carnitine palmitoyltransferase-I activity to accelerate fatty acid β-oxidation, thereby reducing total cholesterol and triglyceride levels in the liver. Thifluzamide also induces hepatotoxicity in zebrafish models and carries a risk of developmental toxicity. Thifluzamide inhibition of Rhizoctonia cerealis may result in low to moderate levels of drug resistance, leading to the generation of stable drug-resistant mutants .
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-
- HY-135446
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders .
|
-
- HY-159641
-
|
BAY-3605349
|
Molecular Glues
Keap1-Nrf2
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors .
|
-
- HY-N0837
-
|
NSC17821; NSC23880
|
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
- HY-W725179
-
|
|
EBV
|
Cancer
|
|
VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
|
-
- HY-15163
-
|
TG02; SB1317
|
JAK
CDK
FLT3
|
Cancer
|
|
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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-
- HY-P10792A
-
|
|
EGFR
|
Cancer
|
|
HYNIC-H6F is a SPECT imaging probe with binding specificity for human epidermal growth factor receptor 2 (HER2) domain II (IC50 = 11 nM). HYNIC-H6F accumulates in HER2-positive breast cancer xenografts via receptor-mediated uptake, while shows low uptake in HER2-negative breast cancer xenografts. HYNIC-H6F enables non-invasive detection of HER2-positive breast cancer in mouse models and allows evaluation of HER2 expression levels without blocking interference. HYNIC-H6F can be used in breast cancer-related research .
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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-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-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 .
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-
- HY-186086
-
|
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Ras
|
Cancer
|
|
RM-041 is a selective, orally active KRAS G13C (ON) inhibitor that forms a covalent complex with KRAS G13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRAS G13C mutant cancer cells. RM-041 induces regression of KRAS G13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer .
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-
- HY-151096
-
|
|
CXCR
|
Inflammation/Immunology
|
|
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research .
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-
- HY-181655
-
|
|
Cathepsin
|
Metabolic Disease
|
|
Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis .
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-
- HY-170824
-
|
|
PROTACs
SWI/SNF Complex
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia .
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-
- HY-B2004R
-
|
|
Reference Standards
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Thifluzamide (Standard) is the analytical standard of Thifluzamide. This product is intended for research and analytical applications. Thifluzamide is a fungicide that inhibits fungal respiration by blocking the ubiquinone-binding site in mitochondrial complex II. Thifluzamide exhibits significant activity against Basidiomycota pathogens (such as Rhizoctonia cerealis, Ustilago and Puccinia genera) and is commonly used in studies on wheat sharp eyespot. Thifluzamide displays a dual mechanism in regulating lipid metabolism: it reduces fatty acid synthase activity to inhibit endogenous fatty acid synthesis, and increases carnitine palmitoyltransferase-I activity to accelerate fatty acid β-oxidation, thereby reducing total cholesterol and triglyceride levels in the liver. Thifluzamide also induces hepatotoxicity in zebrafish models and carries a risk of developmental toxicity. Thifluzamide inhibition of Rhizoctonia cerealis may result in low to moderate levels of drug resistance, leading to the generation of stable drug-resistant mutants .
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-
- HY-186151
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53 null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer .
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-
- HY-117093
-
|
|
HDAC
|
Cancer
|
|
H8-A5 is a novel human histone deacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.
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-
- 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 .
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-
- 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 .
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-
- HY-183741
-
|
|
PI3K
Akt
|
Cancer
|
|
VVD-844 is an orally active covalent inhibitor of PI3Kα inhibitor. VVD-844 covalently binds to Cys 242 in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2-overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers .
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-
- HY-W013403
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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-
- HY-132182
-
HPA-12
1 Publications Verification
|
Ceramidase
Autophagy
Apoptosis
ATF6
|
Neurological Disease
Cancer
|
|
HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .
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-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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-
- HY-NP004
-
|
CVF
|
Complement System
|
Inflammation/Immunology
|
|
Cobra Venom Factor (CVF) is a selective activator targeting complement components C3, C5, and factor B in the complement system. After binding to factor B, Cobra Venom Factor is cleaved by factor D, forming a stable C3/C5 convertase resistant to regulatory proteins H and I. This continuously hydrolyzes C3 and C5, depleting serum complement while inducing neutrophil migration, vascular leakage, and increased TNF-α levels. Cobra Venom Factor can be used to deplete complement and mimic complement activation-related pathological states, and is applied in animal models of complement-mediated diseases such as acute respiratory distress syndrome (ARDS), sepsis, and shock. Cobra Venom Factor can be isolated from the venom of cobras (e.g., Naja atra, Naja melanoleuca, Naja kaouthia, etc.) .
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-
- HY-N7368
-
|
|
Adenosine Deaminase
Bacterial
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
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-
- HY-183246
-
|
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PAK
Cdc42-binding kinase
|
Cancer
|
|
Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr 423/Thr 402/Thr 436 and Ser 141/Ser 144/Ser 154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer .
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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 .
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-
- HY-159922
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC50 value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC50 = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against ARF876L/T877A and ARW741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .
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-
- HY-125938
-
|
Cycloartenol ferulate; Cycloartenol ferulic acid ester
|
Drug Derivative
Apoptosis
Reactive Oxygen Species (ROS)
JAK
STAT
|
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-179372
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50 = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.
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-
- HY-N8146
-
|
|
STAT
Bcl-2 Family
Ser/Thr Kinase
Survivin
c-Myc
Apoptosis
Necroptosis
CDK
|
Infection
Cancer
|
|
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
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-
- HY-12875
-
|
|
Ras
|
Cancer
|
|
BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
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-
- HY-174403
-
|
|
Bcl-2 Family
c-Myc
Apoptosis
Caspase
|
Cancer
|
|
c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
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-
- HY-N7368R
-
|
|
Reference Standards
Adenosine Deaminase
Bacterial
Caspase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Hibifolin (Standard) is the analytical standard of Hibifolin. This product is intended for research and analytical applications. Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
|
-
- HY-N0837R
-
|
NSC17821 (Standard); NSC23880 (Standard)
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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-
- HY-182091
-
|
|
5-HT Receptor
Dopamine Receptor
Dopamine Transporter
Adrenergic Receptor
Calcium Channel
|
Neurological Disease
|
|
CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease .
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-
- HY-P10427A
-
|
|
CXCR
Dengue Virus
|
Infection
|
|
DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA 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 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
|
-
- HY-W008270R
-
|
γ-Crotonolactone (Standard)
|
Reference Standards
Endogenous Metabolite
|
Others
|
|
2(5H)-Furanone (Standard) is the analytical standard of 2(5H)-Furanone. This product is intended for research and analytical applications. 2(5H)-Furanone (γ-Crotonolactone) is an endogenous metabolite. 2(5H)-Furanone mimics N-acyl homoserine lactone signals, occupies the binding site of LuxR homologs, and interferes with quorum sensing-mediated gene regulation. 2(5H)-Furanone inhibits quorum sensing mediated by AHLs with different acyl chain lengths. 2(5H)-Furanone inhibits biofilm formation of environmental Aeromonas hydrophila strains on polystyrene plates. 2(5H)-Furanone suppresses spike-and-wave discharges in a rat model of generalized absence seizures and exhibits selective activity against absence seizures. 2(5H)-Furanone can be used in studies related to bacteria infections and generalized absence seizures.
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-
- HY-175236
-
|
|
PD-1/PD-L1
Apoptosis
ERK
JNK
Cadherin
p38 MAPK
GSK-3
IFNAR
Caspase
Bcl-2 Family
|
Cancer
|
|
SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research .
|
-
- HY-164429
-
|
|
Integrin
Elastase
|
Cancer
|
|
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
|
-
- HY-13032B
-
|
GSK 525762C; I-BET 762 besylate
|
Epigenetic Reader Domain
ERK
|
Cancer
|
|
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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-
- 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)) .
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-
- HY-161483
-
|
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Neurological Disease
Cancer
|
|
CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function .
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-
- HY-W013403S
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-N5112A
-
|
Arnebin 1
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
|
Inflammation/Immunology
|
|
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
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-
- HY-177578
-
|
|
Antibody-Drug Conjugates (ADCs)
c-Kit
Apoptosis
Microtubule/Tubulin
ERK
Akt
Caspase
|
Cancer
|
|
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
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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-182361
-
|
|
AMPK
JAK
Cadherin
|
Cancer
|
|
NUAK1-IN-3 is a potent and selective NUAK1 inhibitor with an IC50 of 0.49 nM. NUAK1-IN-3 also inhibits NUAK2 and JAK3 with IC50 values of 265 and 225 nM. NUAK1-IN-3 engages Glu139 of NUAK1, forms a salt bridge between its bicyclic ring nitrogen and Asp142, and uses a fluorine atom to enhance hydrophobic binding interactions. NUAK1-IN-3 attenuates MYPT1 phosphorylation, suppresses the NUAK1-MYPT1 signaling axis, and inhibits proliferation, migration, and invasion of triple-negative breast cancer cells. NUAK1-IN-3 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) marker alterations, downregulates Snail and N-cadherin, and upregulates E-cadherin in tumor tissues. NUAK1-IN-3 suppresses tumor growth in triple-negative breast cancer xenograft models. NUAK1-IN-3 can be used for the research of triple-negative breast cancer .
|
-
- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
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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-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
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- HY-182360
-
|
|
PERK
Eukaryotic Initiation Factor (eIF)
Bcl-2 Family
Apoptosis
Reactive Oxygen Species (ROS)
STING
DNA/RNA Synthesis
PD-1/PD-L1
|
Cancer
|
|
Cytisine-Platinum(IV) Prodrug-1 is a Pt(IV) prodrug incorporating the natural compound Cytisine (HY-N0175) with antiproliferative activity against tumor cells. Cytisine-Platinum(IV) Prodrug-1 promotes calcium transfer across the IP3R1-GRP75-VDAC1 axis to drive mitochondrial calcium overload. Cytisine-Platinum(IV) Prodrug-1 initiates unfolded protein response via PERK, eIF2α, ATF4, and CHOP to modulate Bcl-2 and Bax, triggering apoptosis. Cytisine-Platinum(IV) Prodrug-1 induces mitochondrial dysfunction, ROS production, reduced ATP synthesis, DNA damage, and S-phase cell cycle arrest. Cytisine-Platinum(IV) Prodrug-1 activates the cGAS-STING pathway, reduces PD-L1 expression, drives immunogenic cell death. Cytisine-Platinum(IV) Prodrug-1 exhibits high physiological stability, efficient cellular accumulation, and enhanced platinum-DNA binding, and inhibits tumor growth in mouse models with reduced systemic toxicity. Cytisine-Platinum(IV) Prodrug-1 can be used for the research of lung cancer .
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-
- 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 .
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-
- 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-NP008
-
|
|
Lipocalin Family
|
Inflammation/Immunology
|
|
β-Lactoglobulin, a major whey protein, is a small globular protein from the lipocalin family. β-Lactoglobulin is an important source of the essential and branched-chain amino acids (leucine, isoleucine, and valine). β-Lactoglobulin shows antioxidant properties, because it contains two disulfide bonds and one free thiol group. β-Lactoglobulin is a ligand transport agent. β-Lactoglobulin is one of the major allergens in milk and can be utilized in the research for developing safe hypoallergenic dairy products .
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-
-
-
HY-L0115V
-
|
|
10,091 compounds
|
|
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.
Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.
|
| Cat. No. |
Product Name |
Type |
-
- HY-164992
-
|
MRG002; Trastuzumab MMAE
|
Fluorescent Dye
|
|
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
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-
- HY-D3192
-
|
|
Fluorescent Dye
|
|
CDy11 is a fluorescent probe and amyloid-binding dye (λex=590 nm; λem=612 nm), with a Ka of 29 μM for Pseudomonas aeruginosa Fap. CDy11 specifically recognizes amyloid fibrils in bacterial biofilms and exhibits significantly enhanced fluorescence upon binding to the target. CDy11 shows no staining effect on amyloid-deficient mutant strains, planktonic cells or protein monomers. CDy11 supports in vivo imaging of Pseudomonas aeruginosa biofilms in mouse implant and corneal infection models. CDy11 is widely used in studies of Staphylococcus aureus biofilm infections, dental caries, and Pseudomonas aeruginosa-associated implant and corneal infections .
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| Cat. No. |
Product Name |
Type |
-
- HY-N0830B
-
|
|
Biochemical Assay Reagents
|
|
Palmitic acid sodium is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid sodium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid sodium is used to establish a cell steatosis model .
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-
- HY-NP008
-
|
|
Biochemical Assay Reagents
|
|
β-Lactoglobulin, a major whey protein, is a small globular protein from the lipocalin family. β-Lactoglobulin is an important source of the essential and branched-chain amino acids (leucine, isoleucine, and valine). β-Lactoglobulin shows antioxidant properties, because it contains two disulfide bonds and one free thiol group. β-Lactoglobulin is a ligand transport agent. β-Lactoglobulin is one of the major allergens in milk and can be utilized in the research for developing safe hypoallergenic dairy products .
|
-
- HY-D0846
-
|
|
Biochemical Assay Reagents
|
|
Diethyl pyrocarbonate is a potent, orally active, non-specific chemical inhibitor of RNase. Diethyl pyrocarbonate has been useful in vitro as an agent relatively specific for binding to imidazole of histidine. Diethyl pyrocarbonate inhibits central chemosensitivity in rabbits. Diethyl pyrocarbonate can modify Ser, Thr, His and Tyr residues. Diethyl pyrocarbonate can be used for modeling .
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-
- HY-NP004
-
|
CVF
|
Biochemical Assay Reagents
|
|
Cobra Venom Factor (CVF) is a selective activator targeting complement components C3, C5, and factor B in the complement system. After binding to factor B, Cobra Venom Factor is cleaved by factor D, forming a stable C3/C5 convertase resistant to regulatory proteins H and I. This continuously hydrolyzes C3 and C5, depleting serum complement while inducing neutrophil migration, vascular leakage, and increased TNF-α levels. Cobra Venom Factor can be used to deplete complement and mimic complement activation-related pathological states, and is applied in animal models of complement-mediated diseases such as acute respiratory distress syndrome (ARDS), sepsis, and shock. Cobra Venom Factor can be isolated from the venom of cobras (e.g., Naja atra, Naja melanoleuca, Naja kaouthia, etc.) .
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-
- HY-NP006
-
|
SPA
|
Biochemical Assay Reagents
|
|
Protein A (SPA) is an immunoglobulin (Ig)-binding protein that exists on the bacterial surface and can be freely secreted into the extracellular environment. Protein A blocks opsonophagocytosis and induces B cell apoptosis in vitro by binding to the Fc region of antibodies and the Fab region of B cell receptors. Protein A can form toxic immune complexes with IgG, thereby inducing leukocyte necrosis. Protein A contributes to the virulence expression of Staphylococcus aureus. Protein A triggers allergic reactions in IgG-pretreated mouse models. Protein A can be used in studies related to immune system diseases .
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-
- HY-W127458
-
|
Hexadecanoic acid, tin(2+) salt
|
Biochemical Assay Reagents
|
|
Tin(II) palmitate (Hexadecanoic acid, tin(2+) salt) is a long-chain saturated fatty acid commonly found in animals and plants. Tin(II) palmitate can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granular cells. Tin(II) palmitate can be used to establish a model of cellular steatosis.
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3732
-
|
|
Integrin
|
Cancer
|
|
RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models .
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-
- HY-P2460
-
|
|
Bacterial
Fungal
Interleukin Related
TNF Receptor
|
Infection
Inflammation/Immunology
|
|
SMAP‑29 is a cathelicidin antimicrobial peptide with LPS‑binding and anti‑inflammatory properties. SMAP‑29 exerts broad‑spectrum antimicrobial activity against bacteria, fungi and multidrug‑resistant isolates. SMAP‑29 kills pathogens by permeabilizing bacterial membranes, inducing depolarization and cell lysis, and also inhibits inflammatory cytokines while reducing lethality in septic shock and pneumonia models. SMAP-29 can be used for research on bacterial infections, drug-resistant infections, septic shock .
|
-
- HY-P5542
-
|
SB-01; Peniel 2000
|
Factor Xa
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases .
|
-
- HY-P10943
-
|
|
Fluorescent Dye
|
Inflammation/Immunology
Cancer
|
|
APO-15 is a phosphatidylserine-binding fluorescent probe and apoptosis imaging reagent. APO-15 exhibits high chemical stability under proteolytic and oxidative conditions, enables quantification and imaging of drug-induced apoptosis in preclinical mouse models, and is applicable to fixed tissue samples and multiple in vivo administration routes (Ex = 488 nm; Em = 525 nm). APO-15 can be used in studies related to acute lung injury and breast cancer .
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-
- HY-P10861A
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease .
|
-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as Alzheimer's disease .
|
-
- 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-P1220A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P10427A
-
|
|
CXCR
Dengue Virus
|
Infection
|
|
DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA 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 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases .
|
-
- HY-P11354
-
|
|
TGF-β Receptor
Apoptosis
Interleukin Related
Integrin
Cadherin
|
Inflammation/Immunology
|
|
THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis .
|
-
- HY-P11354A
-
|
|
TGF-β Receptor
Apoptosis
Interleukin Related
Integrin
Cadherin
|
Inflammation/Immunology
|
|
THR-123 TFA is an orally active ALK3 peptide agonist. THR-123 TFA has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 TFA suppresses inflammation, Apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 TFA can be used for the study of kidney fibrosis .
|
-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
|
-
- HY-P1220
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
|
-
- HY-P10870
-
|
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
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-
- 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-P10010
-
|
|
Galectin
|
Cancer
|
|
DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .
|
-
- HY-P2138
-
|
|
HIV Protease
|
Others
|
|
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-P11618
-
|
|
Glycoprotein VI
|
Cancer
|
|
10P3Me is a Glypican-3 (GPC3)-targeting probe with a Ka of 93.8 nM for the human target. 10P3Me exhibits high binding affinity to GPC3, targets GPC3-positive cells, and serves as an agent for PET imaging. 10P3Me selectively accumulates in GPC3-positive tumor tissues, including subcutaneous xenograft models and orthotopic HepG2-LUC liver cancer models, to achieve precise localization of lesions .
|
-
- 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-P10792A
-
|
|
EGFR
|
Cancer
|
|
HYNIC-H6F is a SPECT imaging probe with binding specificity for human epidermal growth factor receptor 2 (HER2) domain II (IC50 = 11 nM). HYNIC-H6F accumulates in HER2-positive breast cancer xenografts via receptor-mediated uptake, while shows low uptake in HER2-negative breast cancer xenografts. HYNIC-H6F enables non-invasive detection of HER2-positive breast cancer in mouse models and allows evaluation of HER2 expression levels without blocking interference. HYNIC-H6F can be used in breast cancer-related research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P990673
-
|
DSTP-3086S Antibody; RG-7450 Antibody
|
ADC Antibody
Transmembrane Glycoprotein
Mitosis
|
Cancer
|
|
Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
|
-
(5)
-
- HY-P9964
-
|
11F8; IMC-11F8; LY3012211
|
EGFR
|
Cancer
|
|
Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
|
-
(5)
-
- HY-P99171
-
|
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
(5)
-
- HY-P991577
-
|
DS-8895A
|
Ephrin Receptor
|
Cancer
|
|
DS-8895(DS-8895A) is an anti-EphA2 monoclonal antibody with specific binding to EphA2 receptors and EphA2-expressing cells. DS-8895, when conjugated with 89Zr, 111In, or 125I, supports molecular imaging of EphA2 expression in xenograft models. DS-8895 allows noninvasive measurement of EphA2 expresssion in tumors in vivo. .
|
-
(5)
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
(5)
-
- HY-P991598
-
|
MOR12743; MOR03207
|
Interleukin Related
NF-κB
|
Inflammation/Immunology
|
|
MOR-106 (MOR12743) is a humanized anti-IL-17C IgG1 monoclonal antibody. MOR-106 inhibits the NF-κB signaling pathway by specifically binding to IL-17C (IC50 = 59 pM for human IL-17C, IC50 = 55 pM for mouse IL-17C). MOR-106 can effectively inhibit skin inflammation and reduce related inflammatory factors in animal models of psoriasis and atopic dermatitis .
|
-
(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-P99249
-
|
Pogalizumab; MOXR 0916
|
Orexin Receptor (OX Receptor)
|
Cancer
|
|
Vonlerolizumab (Pogalizumab; MOXR 0916) is a humanized IgG1 monoclonal antibody targeting OX40 (CD134). Pogalizumab partially blocks the interaction between OX40 and its natural ligand OX40L upon binding, thereby activating the NF-κB signaling pathway. Pogalizumab enhances T cell activation and proliferation and has shown antitumor activity in mouse models .
|
-
(5)
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
(5)
-
- HY-P990004
-
|
|
Tim3
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse TIM-3 Antibody (B8.2C12) is an anti-mouse TIM-3 IgG1 monoclonal antibody. Anti-Mouse TIM-3 Antibody (B8.2C12) can block the binding of Tim-3 with Phosphatidylserine (PtdSer) and CEACAM1 without interfering with the binding to Galectin-9. Anti-Mouse TIM-3 Antibody (B8.2C12) can inhibit tumor growth and activate tumor infiltrating CD8 + T cells. Anti-Mouse TIM-3 Antibody (B8.2C12) can be used for studying cancer such as breast cancer and colon cancer and constructing experimental autoimmune encephalomyelitis (EAE) 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-P991447
-
|
|
VISTA
|
Cancer
|
|
Anti-VSIR/VISTA Antibody (SG7) is a human monoclonal antibody (mAb) targeting VISTA/B7-H5. Anti-VSIR/VISTA Antibody (SG7) inhibits VISTA function and prevents PSGL-1 and VSIG3 from binding to VISTA. Anti-VSIR/VISTA Antibody (SG7) has anti-tumor activity in the mouse B16F10 melanoma model. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P990778
-
|
ATG-101
|
TNF Receptor
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
Xirestomig (ATG-101) is a tetravalent "2+2″ PD-L1×4-1BB bispecific antibody. Xirestomig binds PD-L1 and 4-1BB concurrently, with a greater affinity for PD-L1, and potently activated 4-1BB+ T cells when cross-linked with PD-L1-positive cells. Xirestomig activates exhausted T cells upon PD-L1 binding. Xirestomig displays potent antitumor activity in numerous in vivo tumor models, including those resistant or refractory to immune checkpoint inhibitors (ICIs) .
|
-
(5)
-
- HY-P991618
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
ST2485 is a monoclonal antitenascin antibody. ST2485 shows additivity in tenascin C binding in vitro as well as in a xenograft model. ST2485 binds human tenascin at an epitope partially shared with BC2. ST2485 cross-reacts with murine tenascin. ST2485 can be studied in antitumor research .
|
-
(5)
-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
(5)
-
- HY-145644
-
|
C-135-LS; BMS-986414
|
SARS-CoV
|
Infection
Cancer
|
|
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
|
-
(5)
-
- HY-P991353
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models .
|
-
(5)
-
- HY-P991270
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
|
-
(5)
-
- HY-P992474
-
|
|
Interleukin Related
STAT
CCR
Fc Receptor (FcR)
|
Inflammation/Immunology
|
|
TAVO101 is a humanized anti-TSLP antibody with an EC50 of 0.19 nM against hTSLP. TAVO101 inhibits STAT5 activation and CCL17 release. TAVO101 carries Fc region mutations that enhance its binding to FcRn while reducing its binding to FcγRI, FcγRIIIA and C1q, thereby attenuating effector functions. TAVO101 reduces the levels of inflammatory markers, cell infiltration and histopathological damage in preclinical models of asthma, psoriasis and atopic dermatitis. TAVO101 can be used for research related to asthma, psoriasis and atopic dermatitis .
|
-
(5)
-
- HY-P992473
-
|
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
TAS266 is a tetrameric nanobody agonist targeting DR5. TAS266 selectively induces cancer cell death. TAS266 triggers sustained tumor regression in xenograft models and also elicits immunogenic responses including antibody binding. TAS266 exhibits superior anti-tumor efficacy compared with traditional DR5-targeting strategies. TAS266 can be used in research related to pancreatic cancer and advanced solid tumors .
|
-
(5)
-
- HY-P992342
-
|
|
Tim3
|
Cancer
|
|
DCB-8 is a specific inhibitor targeting human TIM-3. DCB-8 regulates T cell function, enhances cytokine secretion, and inhibits tumor growth in disease animal models. DCB-8 can be used for cancer research .
|
-
(5)
-
- HY-P992066
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
|
|
Anti-Mouse DDR2 Antibody (DAB0065) is a mAb that specifically targets mouse discoidin domain receptor DDR2 without cross-reacting with DDR1. Anti-Mouse DDR2 Antibody (DAB0065) binds to the extracellular domain of native mouse DDR2, induces endocytosis and lysosomal degradation of DDR2, and this process is independent of collagen binding. Anti-Mouse DDR2 Antibody (DAB0065) exhibits significant therapeutic effects in both the unilateral ureteral obstruction (UUO) mouse model of renal fibrosis and the bleomycin (HY-108345)-induced mouse model of pulmonary fibrosis, effectively downregulating the mRNA expression of type I collagen Col1a1 and fibronectin Fn1. Anti-Mouse DDR2 Antibody (DAB0065) can be humanized and has the potential to be developed as a targeted agent for diseases such as idiopathic pulmonary fibrosis and renal fibrosis .
|
-
(5)
-
- HY-P992082
-
|
|
VEGFR
|
Cancer
|
|
Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF . The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
(5)
-
- HY-P992388
-
|
|
LILRB
|
Cancer
|
|
IO-108 is a humanized IgG4 monoclonal antibody and a competitive inhibitor of LILRB2, with a KD value of 1.97 nM. IO-108 competitively blocks the binding of LILRB2 to its ligands including HLA-G, MHC-I, ANGPTL2 and SEMA4A, reprograms tumor-associated myeloid cells, drives the conversion of suppressive myeloid cells into a pro-inflammatory phenotype, and restores the cytotoxic activity of T cells and NK cells. IO-108 inhibits tumor growth in LILRB2 transgenic mouse models. IO-108 can be used for the research of solid tumors .
|
-
(5)
-
- HY-P992062
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
|
|
Anti-Mouse CD80 Antibody (TKMG48) is an antibody that targets mouse CD80. By specifically binding to and disrupting the CD80:PD-L1 complex to release PD-L1, Anti-Mouse CD80 Antibody (TKMG48) functions as an indirect PD-1 agonist without blocking CD28 co-stimulation or CD80-CTLA4 binding. Anti-Mouse CD80 Antibody (TKMG48) inhibits T cell activation, reduces T cell effector functions and antigen-specific CD8 + T cell populations, and does not interfere with the differentiation, migration, antigen presentation or surface marker expression of dendritic cells. Anti-Mouse CD80 Antibody (TKMG48) significantly attenuates disease severity in mouse models of arthritis, spondyloarthritis, multiple sclerosis and Sjögren's syndrome, and its activity depends on the expression of PD-1 and PD-L1 .
|
-
(5)
-
- HY-P992449
-
|
PRLR ADC antibody
|
ADC Antibody
|
Cancer
|
|
REGN2878 (PRLR ADC antibody) is a monoclonal antibody targeting the prolactin receptor (PRLR) and can block prolactin‑mediated activation of PRLR. REGN2878 exhibits an equilibrium dissociation constant (KD) of 1.05 nM and an IC50 of 0.344 nM for human PRLR. REGN2878 can be rapidly internalized and degraded in lysosomes by PRLR‑positive tumor cells, showing antigen‑specific binding and targeted enrichment properties. REGN2878 derivatives can be used as an immunoPET agent for antigen‑specific imaging of PRLR‑related tumors, and can also serve as a component of ADCs to exert anti‑tumor activity in breast cancer xenograft models. REGN2878 can be used in the research of breast cancer and prostate cancer. Isotype Comparison HY-P99001 .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0830
-
-
-
- HY-B0470
-
-
-
- HY-N0837
-
|
NSC17821; NSC23880
|
Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Classification of Application Fields
Plants
Disease Research Fields
Source Classification
Cancer
|
PI3K
Akt
mTOR
Autophagy
Apoptosis
|
|
Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
|
-
-
- HY-N7368
-
|
|
Flavonols
Flavonoids
other families
Neurological Disease
Classification of Application Fields
Phenols
Polyphenols
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Adenosine Deaminase
Bacterial
Caspase
|
|
Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
|
-
-
- 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-B1864A
-
-
-
- HY-107830
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Metabolic Disease
Disease Research Fields
Steroids
Source Classification
|
Endogenous Metabolite
Collagen
|
|
Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
|
-
-
- HY-W008270
-
-
-
- HY-N5112A
-
|
Arnebin 1
|
Quinones
Structural Classification
other families
Classification of Application Fields
Other Diseases
Plants
Naphthalene Quinones
Pteris livida Mett.
Disease Research Fields
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
|
|
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
|
-
-
- 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 .
|
-
-
- HY-N8146
-
-
-
- HY-N0837R
-
|
NSC17821 (Standard); NSC23880 (Standard)
|
Alkaloids
Piperidine Alkaloids
Structural Classification
other families
Plants
Source Classification
|
Reference Standards
PI3K
Akt
mTOR
Autophagy
Apoptosis
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Veratramine (NSC17821; NSC23880) (Standard) is the analytical standard of Veratramine (HY-N0837). This product is intended for research and analytical applications. Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy .
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- HY-N0830A
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- HY-B1864AR
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- HY-N1486R
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- HY-107830R
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Structural Classification
Microorganisms
Steroids
Source Classification
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Reference Standards
Endogenous Metabolite
Collagen
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Methyl cholate (Standard) is the analytical standard of Methyl cholate. This product is intended for research and analytical applications. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
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- HY-N11768
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- HY-N7368R
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Flavonols
Structural Classification
Flavonoids
other families
Phenols
Polyphenols
Plants
Source Classification
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Reference Standards
Adenosine Deaminase
Bacterial
Caspase
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Hibifolin (Standard) is the analytical standard of Hibifolin. This product is intended for research and analytical applications. Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A) .
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- HY-W008270R
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γ-Crotonolactone (Standard)
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Structural Classification
Natural Products
Endogenous metabolite
Source Classification
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Reference Standards
Endogenous Metabolite
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2(5H)-Furanone (Standard) is the analytical standard of 2(5H)-Furanone. This product is intended for research and analytical applications. 2(5H)-Furanone (γ-Crotonolactone) is an endogenous metabolite. 2(5H)-Furanone mimics N-acyl homoserine lactone signals, occupies the binding site of LuxR homologs, and interferes with quorum sensing-mediated gene regulation. 2(5H)-Furanone inhibits quorum sensing mediated by AHLs with different acyl chain lengths. 2(5H)-Furanone inhibits biofilm formation of environmental Aeromonas hydrophila strains on polystyrene plates. 2(5H)-Furanone suppresses spike-and-wave discharges in a rat model of generalized absence seizures and exhibits selective activity against absence seizures. 2(5H)-Furanone can be used in studies related to bacteria infections and generalized absence seizures.
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- HY-N0493R
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Structural Classification
Flavonoids
Flavones
Campylotropis hirtella (Franch.) Schindl.
Phenols
Polyphenols
Plants
Compositae
Source Classification
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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-N17727
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Product Name |
Chemical Structure |
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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-W757743
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Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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- HY-N0830S22
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Palmitic acid- 13C-1 is the 13C-labeled Palmitic acid (HY-N0830). Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells. Palmitic acid is used to establish a cell steatosis model .
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- HY-W746556
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Methyl cholate-d5 is the deuterium labeled Methyl cholate. Methyl cholate is a bile acid analog and a specific inhibitor of TcdB toxin from Clostridioides difficile. Methyl cholate exerts a stronger selective inhibitory effect on TcdB than on TcdA. Methyl cholate induces conformational stabilization by binding to a unique site of TcdB, thereby blocking the binding of the toxin to host receptors and its self-processing process. Methyl cholate effectively protects human fibroblasts from TcdB-induced cytopathic effects. Methyl cholate exhibits dose-dependent anti-hepatic fibrosis activity in both cellular and zebrafish models, and significantly reduces the expression levels of α-SMA and COL-I. Methyl cholate is suitable for in-depth research in the fields of Clostridioides difficile infection and hepatic fibrosis .
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- HY-W013403S
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2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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Product Name |
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Classification |
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- HY-175421
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Alkynes
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ArMan is an aryl mannoside ligand that can be chemically functionalized onto the surface of virus-like particles (VLPs) through click chemistry. VLPs can be used to target DC-SIGN dendritic cells, promote the selective co-binding of DC-SIGN and TLR7, and lead to a Th1-type immune response. VLP-ArMan-OvaI/II can significantly inhibit tumor growth in the mouse melanoma model .
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Product Name |
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Classification |
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- HY-147081
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AS 1411
2 Publications Verification
AGRO-100
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Aptamers
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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- HY-112974
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GSK-2998728; ISIS-420915
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Antisense Oligonucleotides
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Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy .
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- HY-W140439
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18:1 Lyso PC
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Phospholipids
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1-Oleoyl-sn-glycero-3-phosphocholine (18:1 Lyso PC), a lysophospholipid, is a GPR82 inhibitor. 1-Oleoyl-sn-glycero-3-phosphocholine abrogates constitutive Gi-coupled GPR82 activity, shifts active/inactive equilibrium to inactive, suppresses Gi protein activation, increases cAMP production, and decreases GTPγS binding to Gαi proteins. 1-Oleoyl-sn-glycero-3-phosphocholine contributes to adipocyte lipolysis regulation.1-Oleoyl-sn-glycero-3-phosphocholine exhibits reduced serum levels in mouse models of steatohepatitis, linked to hepatic Lpcat 1-4 up-regulation .
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- HY-147081A
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AGRO-100 sodium
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Aptamers
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AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
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