Search Result
Results for "
mouse model
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
9
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-149464
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Ras
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Cancer
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ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model .
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- HY-N12840
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Others
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Metabolic Disease
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Logmalicid B is an iridoid glycoside compound that can be isolated from Cornus officinalis and can be used in diabetes research .
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- HY-122120
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AJ‐9677
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Adrenergic Receptor
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Metabolic Disease
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Rafabegron (AJ-9677) is a specific beta3-adrenoceptor agonist. Rafabegron can reduce blood glucose, insulin, FFA, and triglyceride levels in diabetic and obese mouse models .
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- HY-P4253
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VEGFR
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Cardiovascular Disease
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Arginyl-Glutamine is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy .
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- HY-P5183
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Sodium Channel
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Neurological Disease
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Hm1a is a disulfide-rich spider-venom peptide, and a NaV1.1 activator. Hm1a restores the function of inhibitory interneurons in Dravet syndrome (DS) mouse model .
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- HY-P3350
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Bacterial
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Infection
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LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
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- HY-157958
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nAChR
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Neurological Disease
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α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model .
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- HY-156123
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Dihydrofolate reductase (DHFR)
Bacterial
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Infection
Cancer
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DHFR-IN-9 (compound 8A) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-9 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=0.25 μg/mL) and has anti-infective effects in mouse models of systemic infection and thigh infection caused by it (dose: 2.5 mg /kg, 5 mg/kg; ip). DHFR-IN-9 has stronger anticancer activity than paclitaxel (Y-B0015) in a mouse model of breast cancer (dose: 2.5 mg/kg; ip; once every 3 days) .
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- HY-163076
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Others
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Others
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Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
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- HY-156122
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Dihydrofolate reductase (DHFR)
Bacterial
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Infection
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DHFR-IN-8 (compound 6r) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-8 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=15.6 ng/mL) in mouse models of systemic infection and thigh infection .
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- HY-146465
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Microtubule/Tubulin
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Cancer
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Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC50 = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model .
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- HY-156430
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MMP
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Cancer
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MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
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- HY-162315
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MAGL
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Neurological Disease
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MAGL-IN-16 (compound 27) is an oral active, selective and reversible MAGL inhibitor with the IC50 value of 10.3 nM. MAGL-IN-16 can increase the level of 2-AG and shows antidepressant effect in mouse depressed model caused by chronic restraint stress .
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- HY-155079
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EGFR
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Cancer
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DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
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- HY-N7922
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Decarboxyellagic acid
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Influenza Virus
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Infection
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Urolithin M5 is a neuraminidase inhibitor that can be isolated from Ganlanye. Urolithin M5 has antiviral activity in vitro and in vivo by inhibiting the activity of viral NA. Urolithin M5 can increase the survival rate and improve pulmonary edema in pr8-infected mouse models. Urolithin M5 can be used in anti-influenza research .
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- HY-16384
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Antibiotic L 156602; PD 124966
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Complement System
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Inflammation/Immunology
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L-156602 is a C5a receptor antagonist. L-156602 inhibits inflammation, and the migration of monocytes and neutrophils to the infiltrating site in mouse inflammatory models. L-156602 suppresses the efferent phase of delayed-type hypersensitivity (DTH) .
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- HY-149949
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Apoptosis
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Cancer
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Anticancer agent 105 is a compound based on thienopyrimidine scaffold, with with good safety and anticancer properties. Anticancer agent 105 shows selective toxicity towards melanoma cancer, and induces apoptosis. And Anticancer agent 105 significantly inhibits the metastatic nodules, even in pulmonary metastatic melanoma mouse model .
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- HY-155659
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Nuclear Hormone Receptor 4A/NR4A
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Neurological Disease
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4A7C-301 is a Nurr1 agonist with robust neuroprotective effects in vitro. 4A7C-301 significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models. 4A7C-301 can be used for the research of Parkinson’s disease .
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- HY-155417
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Others
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Neurological Disease
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GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
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- HY-145239
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model .
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- HY-151928
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JNK
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Neurological Disease
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JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
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- HY-155820
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NF-κB
NO Synthase
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
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- HY-155821
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NF-κB
NO Synthase
TNF Receptor
Interleukin Related
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Inflammation/Immunology
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Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model .
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- HY-160587
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SRPK
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Cardiovascular Disease
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Antiangiogenic agent 5 (compound 17) has anti-angiogenic activity. Antiangiogenic agent 5 show inhibition to SRPK1, with IC50 of 1.3 nM .
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- HY-12788
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- HY-50884
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- HY-139668
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Neurotensin Receptor
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Cancer
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VGD071, a sortilin-targeting compound, is a promising candidate for future studies using mouse breast cancer models.
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- HY-B1899
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Endogenous Metabolite
Apoptosis
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Neurological Disease
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Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
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- HY-101459
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Others
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Metabolic Disease
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RTC13 restores dystrophin expression and improves muscle function in the mdx mouse model for Duchenne muscular dystrophy (DMD) .
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- HY-109010
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HM71224; LY3337641
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Btk
BMX Kinase
Toll-like Receptor (TLR)
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Metabolic Disease
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Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis .
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- HY-153364
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PPAR
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Cancer
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FTX-6746 is an orally active PPARG inhibitor. FTX-6746 shows potent tumor inhibition in mouse xenograft models .
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- HY-N0648
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Others
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Inflammation/Immunology
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Monotropein is an iridoid glycoside isolated Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model .
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- HY-P1727
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YAP
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Cancer
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Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
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- HY-W764758
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Aryl Hydrocarbon Receptor
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Inflammation/Immunology
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3-OH-Kynurenamine dihydroiodide is the dihydroiodide form of 3-OH-Kynurenamine (HY-156908). 3-OH-Kynurenamine dihydroiodide is an activator for aryl hydrocarbon receptor (AhR), and thus regulates the immune response. 3-OH-Kynurenamine dihydroiodide upregulates the expressions of Ido1 and Tgfb1, ameliorates the skin inflammation in psoriasis mouse model and kidney damage in nephrotoxic lupus mouse model .
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- HY-P99578
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HL036337; HBM9036
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TNF Receptor
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Others
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Tanfanercept (HL036337) is an anti-TNF-α monoclonal antibody. Tanfanercept is effective in ameliorating corneal erosions in a dry eye (DE) mouse model .
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- HY-B1899S
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Isotope-Labeled Compounds
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Others
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Taurodeoxycholic acid-d5is the deuterium labeledTaurodeoxycholic acid(HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
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- HY-12182
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Prostaglandin Receptor
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Cancer
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ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
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- HY-P1727A
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YAP
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Cancer
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Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model .
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- HY-137992
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Others
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Inflammation/Immunology
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Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (BLM)-induced lung fibrosis mouse model. Anti-inflammatory activity .
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- HY-139716
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NF-κB
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Inflammation/Immunology
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IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
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- HY-153521
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BCL6
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Cancer
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CCT374705 is an orally active BCL6 inhibitor with potent antiproliferative effects in vitro. CCT374705 effectively inhibits tumor growth in a lymphoma xenograft mouse model .
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- HY-133898
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TAK-925
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Orexin Receptor (OX Receptor)
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Others
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Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
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- HY-152632
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Cholinesterase (ChE)
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Neurological Disease
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BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC50 values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things .
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- HY-163081
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PARP
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Cancer
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PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
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- HY-163192
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ROR
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Cancer
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W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer .
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- HY-157839
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α-synuclein
Tau Protein
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Neurological Disease
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PROTAC α-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with EC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-synuclein degrader 6 plays an important role in neurodegenerative diseases (NDs) research .
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- HY-17035
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Parasite
Antibiotic
Bacterial
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Infection
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Doramectin is a derivative of Ivermectin (HY-15310). Doramectin is a potent antiparasitic antibiotic. Doramectin is an active compound against S.mansoni in an NMRI mouse infection model .
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- HY-N2195
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(+)-Nootkatone
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Others
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Neurological Disease
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Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects . Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease .
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- HY-P2287
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CRFR
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Neurological Disease
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Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an EC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive agent in the mouse model .
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- HY-147784
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Btk
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Cancer
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HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
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- HY-155146
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Necroptosis
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Cancer
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Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
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- HY-12182A
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Prostaglandin Receptor
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Cancer
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ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
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- HY-P1787
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Amyloid-β
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Neurological Disease
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β-Amyloid (4-10) is an epitope for the polyclonal anti-Aβ(1-42) antibody, reduces amyloid deposition in a transgenic Alzheimer disease mouse model .
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- HY-136447
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ASP4132
1 Publications Verification
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AMPK
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Cancer
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ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
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- HY-111258
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- HY-153996
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Deubiquitinase
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Cancer
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CT1113 is a potent USP28 and USP25 inhibitor. CT1113 decreases the MYC level in vivo，exhibits anti-tumor activity in mouse pancreatic cancer CDX model .
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- HY-120924
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- HY-128901
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F 14679 fumarate
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5-HT Receptor
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Neurological Disease
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F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress .
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- HY-147136
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Others
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Cancer
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MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration .
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- HY-131420
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Aseanostatin P1; Isotetradecanoic acid
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Biochemical Assay Reagents
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Others
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12-Methyltridecanoic acid is a methylated fatty acid that has been found in milk. 12-Methyltridecanoic acid (200 μM) reduces angiogenesis and corneal opacity in alkaline or Pseudomonas aeruginosa-induced ocular mouse models.
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- HY-153670
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CCR
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Cancer
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IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
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- HY-162042
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AMPK
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Metabolic Disease
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AMPK activator 14 (compound 32) is an orally active AMPK activator. AMPK activator 14 decreases fasted glucose and insulin levels in a db/db mouse model of Type II diabetes .
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- HY-163069
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Bacterial
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Infection
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Antitubercular agent-43 (compound A11) is an orally active and potent antitubercular agent. Antitubercular agent-43 shows highly metabolic stability against human and mouse cytochrome P450 enzymes. Antitubercular agent-43 exhibits bactericidal efficacy in acute TB infection mouse model .
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- HY-U00442
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CTX1
1 Publications Verification
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MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system .
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- HY-13646C
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HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride
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P-glycoprotein
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Cancer
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Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models .
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- HY-111209
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S14161
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PI3K
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Cancer
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Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research .
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- HY-15782
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Others
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Cancer
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YH16899 binds Lysyl-tRNA synthetase (KRS), and inhibits membrane translocation of KRS. YH16899 impares the interaction of KRS with 67LR. YH16899 inhibits tumor metastasis in mouse models .
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- HY-126242S
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JAK
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Inflammation/Immunology
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Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].
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- HY-146054
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CXCR
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Inflammation/Immunology
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CXCR4 modulator-2 (compound Z7R) is a highly potent CXCR4 modulator with an IC50 value of 1.25 nM. CXCR4 modulator-2 has acceptable stability (t1/2 = 77.1 min) in mouse serum and exhibits anti-inflammatory activity in mouse edema model .
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- HY-16706
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Histone Acetyltransferase
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Cancer
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Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
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- HY-124733A
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Oxytocin Receptor
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Neurological Disease
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LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism .
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- HY-155163
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- HY-156881
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Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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PARG-IN-4 (Formula (A)) is an orally active and cell-permeable PARG inhibitor. PARG-IN-4 effectively inhibits tumor growth in mouse models. PARG-IN-4 can be used in cancer research .
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- HY-149539
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FLT3
RET
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Cancer
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PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
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- HY-15582
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Microtubule/Tubulin
ADC Cytotoxin
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Cancer
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Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
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- HY-153254
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus .
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- HY-15323
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P505-15 Hydrochloride
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Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
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Cancer
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PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
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- HY-126379
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Apoptosis
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Cancer
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CDDO-2P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-2P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model .
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- HY-105296
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Sigma Receptor
mAChR
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Cancer
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Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
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- HY-137655
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|
|
Protein Arginine Deiminase
|
Cancer
|
|
BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model .
|
-
- HY-N2556
-
|
|
Others
|
Inflammation/Immunology
|
|
Tirucallol, a tetracyclic triterpene, is isolated from Euphorbia lacteal latex. Tirucallol has topical anti-inflammatory effect. Tirucallol can suppress ear edema in the mouse model and inhibit nitrite production in lipopolysaccharide-stimulated macrophages .
|
-
- HY-N3312
-
|
|
Endogenous Metabolite
|
Infection
|
|
Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
|
-
- HY-145704
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria .
|
-
- HY-153189
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research .
|
-
- HY-N8730
-
|
|
Others
|
Neurological Disease
|
|
7,8,3 ',4 '-Tetramethoxyflavone is an extract
isolated from natural pomegranate juice and seeds. 7,8,3 ',4' -Tetramethoxyflavone has a protective effect on the neurotoxicity of
paraquat-induced Parkinson's disease mouse model .
|
-
- HY-161065
-
|
|
Bacterial
|
Infection
|
|
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection .
|
-
- HY-15324
-
|
P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
|
Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
|
Cancer
|
|
PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
|
-
- HY-150233
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .
|
-
- HY-N0109
-
|
Rhodioloside
|
PINK1/Parkin
mTOR
Apoptosis
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
|
-
- HY-111145
-
|
|
Androgen Receptor
|
Cancer
|
|
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
|
-
- HY-148772
-
|
|
Others
|
Neurological Disease
|
|
PTC258 is a specific and orally active splicing modulator of Elongator complex protein 1 gene (ELP1). PTC258 increases the expression of ELP1 in vitro and in vivo. PTC258 is well tolerated in mouse model .
|
-
- HY-114360A
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
|
-
- HY-123059
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
(Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease .
|
-
- HY-162144
-
|
|
Bacterial
|
Infection
|
|
BDM91288 is an orally active AcrB efflux pump inhibitor of pyridinium piperazine. BDM91288 can enhance the in vivo efficacy of levofloxacin (HY-B0330) in the treatment of Klebsiella pneumoniae pulmonary infection in mouse models .
|
-
- HY-16706A
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
|
-
- HY-136527
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .
|
-
- HY-117709
-
|
|
HDAC
|
Neurological Disease
|
|
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .
|
-
- HY-105321
-
|
PBT 2
|
Bacterial
|
Neurological Disease
|
|
PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria .
|
-
- HY-137440A
-
|
TAK-994
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Firazorexton hydrate (TAK-994) is a potent, brain-penetrant, and orally active orexin type 2 receptor (OX2R) agonist (EC50: 19 nM). Firazorexton hydrate inhibits fragmentation of wakefulness and cataplexy-like episodes in mouse models of narcolepsy .
|
-
- HY-149430
-
|
|
Amyloid-β
|
Neurological Disease
|
|
YIAD-0205 is an orally available Aβ(1?42) aggregation inhibitor. YIAD-0205 demonstrated in vivo efficacy in an AD transgenic mouse model with five familial AD mutations (5XFAD) .
|
-
- HY-P5907
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-163149
-
|
|
HBV
|
Infection
|
|
AB-452, a Dihydroquinolizinone (DHQ) analogue, is a potent and orally active HBV RNA destabilizer. AB-452 inhibits PAPD5/7 proteins in vitro with good in vivo efficacy in a chronic HBV mouse model .
|
-
- HY-B1606
-
|
Chlorthymol; 6-Chlorothymol
|
GABA Receptor
|
Neurological Disease
|
|
Chlorothymol (Chlorthymol) is a potent GABAA receptor subunit, LGC-37, inhibitor. Chlorothymol is an effective anticonvulsant. Chlorothymol is protective in several mouse seizure assays, including the 6-Hz 44-mA model of pharmacoresistant seizures .
|
-
- HY-158160
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
|
-
- HY-126328
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis .
|
-
- HY-114409
-
|
|
Galectin
|
Cancer
|
|
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model .
|
-
- HY-124628
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
|
-
- HY-124733
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism .
|
-
- HY-131004
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
|
-
- HY-148839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research .
|
-
- HY-155250
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis .
|
-
- HY-162239
-
|
|
Others
|
Cancer
|
|
Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
|
-
- HY-163386
-
|
|
Biochemical Assay Reagents
|
Others
|
|
HFTC-HClO 1 is a stable and sensitive ratiometric probe, which images the endogenous HClO. HFTC-HClO 1 exhibits a main emission peak at 579 nm. HFTC-HClO-1 visualizes HClO generated in the rheumatoid arthritis mouse model .
|
-
- HY-A0143
-
-
- HY-P1728
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-137655A
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model .
|
-
- HY-143464
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease .
|
-
- HY-153482
-
|
|
Small Interfering RNA (siRNA)
|
Cancer
|
|
ATU027 is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
|
-
- HY-153482A
-
|
|
Small Interfering RNA (siRNA)
|
Cancer
|
|
ATU027 sodium is a siRNA, which silences expression of protein kinase N3 (PKN3) in the vascular endothelium. ATU027 sodium has previously been shown to inhibit local tumor invasion as well as lymph node and pulmonary metastasis in mouse cancer models.
|
-
- HY-B0702
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-111054A
-
|
MDCG sodium
|
Endogenous Metabolite
|
Others
|
|
N-methyl-N-dithiocarboxyglucamine (MDCG) sodium mobilizes and promotes excretion of metallothionein-bound 109Cd in mouse model. N-methyl-N-dithiocarboxyglucamine significantly lowers the Cd content of both the liver and kidney, which is organs most susceptible to Cd-induced toxicity .
|
-
- HY-12788A
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(S)-PF-04449613 is the left-handed isomer of PF-04449613 (HY-12788). PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM. PF-04449613 improves motor learning ability in a mouse model .
|
-
- HY-156111
-
|
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
|
-
- HY-163159
-
-
- HY-145280
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active .
|
-
- HY-144265
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-5 (compound 33a) is a potent and selective PDE4 inhibitor (IC50=3.1 nM). PDE4-IN-5 has favorable skin permeability and a well-characterized binding mechanism. Anti-psoriasis effect .
|
-
- HY-145280A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active .
|
-
- HY-149700
-
|
|
ROCK
MMP
STAT
|
Others
|
|
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model .
|
-
- HY-118282
-
|
|
PGE synthase
|
Endocrinology
|
|
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice .
|
-
- HY-148258
-
-
- HY-10596
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model .
|
-
- HY-155642
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
PU-48 is a potent urea transporters A (UT-A) inhibitor (IC50=0.32 μM). PU-48 has a good diuretic effect in mouse models, and shows little or no cytotoxicity. PU-48 has the potential to be developed as a diuretic .
|
-
- HY-155109
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-114 is a potent stimulator of interferon genes (STING) agonist. Antitumor agent-114 activates immunity and reduces tumor volume in a mouse model of breast cancer. Antitumor agent-114 can be used for immunity and cancer diseases research .
|
-
- HY-124875
-
|
HIF inhibitor 64B
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
|
|
Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .
|
-
- HY-B0149S3
-
|
Cyclocapron-13C2,15N
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
|
-
- HY-158093
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages .
|
-
- HY-100827
-
|
LF22-0542
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
|
-
- HY-155946
-
|
Sac-1004
|
Others
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
CU06-1004 (Sac-1004) is an orally active endothelial dysfunction blocker. CU06-1004 ameliorates endothelial dysfunction by inhibiting hyperpermeability and inflammation, and is potent in inhibiting vascular leakage and inflammation in various animal models, such as diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. CU06-1004 ameliorates CDAA-induced mouse model of NASH. CU06-1004 also improves cardiac function .
|
-
- HY-14833
-
|
TP300
|
Topoisomerase
|
Cancer
|
|
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
|
-
- HY-P1728A
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-16726
-
|
CG100649
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-P99351
-
|
Anti-MMP9 Reference Antibody (andecaliximab)
|
MMP
|
Cancer
|
|
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-108678
-
|
|
Oxytocin Receptor
Vasopressin Receptor
|
Neurological Disease
|
|
TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models .
|
-
- HY-135217
-
|
|
Apoptosis
|
Cancer
|
|
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model .
|
-
- HY-122989
-
|
|
DYRK
|
Inflammation/Immunology
|
|
Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models .
|
-
- HY-131902
-
|
|
MALT1
|
Cancer
|
|
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse .
|
-
- HY-114483
-
AES-135
1 Publications Verification
|
HDAC
|
Cancer
|
|
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM .
|
-
- HY-108527
-
|
|
RAR/RXR
|
Cancer
|
|
CD1530 is a selective RARγ agonist with an Kd of 150 nM . CD1530 has been used in combination with bexarotene to inhibit oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide in a mouse model of human oral-cavity and esophageal squamous-cell carcinoma .
|
-
- HY-149035
-
|
|
Others
|
Cancer
|
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
|
-
- HY-136990
-
|
|
Others
|
Cancer
|
|
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells .
|
-
- HY-117366
-
|
|
PKC
|
Cancer
|
|
PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613)
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-N2707
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Cancer
|
|
6-Deoxyjacareubin is a natural xanthone, that can be isolated from the leaves of Vismia latifolia. 6-Deoxyjacareubin protects against non-apoptotic cell death by inhibiting ROS production. 6-Deoxyjacareubin ameliorates neurodegeneration in a mouse model of familial amyotrophic lateral sclerosis (ALS) .
|
-
- HY-149708
-
|
|
ICMT
|
Others
|
|
UCM-13207 (compound 21) is a selective ICMT inhibitor that ameliorates basic progeria-like features. UCM-13207 can improve the survival rate of LmnaG609G/G609G mice in the mouse premature aging model .
|
-
- HY-13508
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory .
|
-
- HY-147936
-
|
|
MMP
|
Inflammation/Immunology
|
|
TP0556351 is a potent and selective matrix metalloproteinase-2 (MMP2) inhibitor with an IC50 value of 0.2 nM. TP0556351 reduces the amount of collagen in the lungs of a Bleomycin-induced pulmonary fibrosis mouse model. TP0556351 can be used for researching idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-160021
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
|
-
- HY-152293
-
|
|
VEGFR
ERK
|
Cancer
|
|
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
|
NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
|
-
- HY-N0830
-
-
- HY-142520
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .
|
-
- HY-W016868
-
|
|
Others
|
Metabolic Disease
|
|
3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity .
|
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-N0830B
-
|
|
Biochemical Assay Reagents
HSP
Endogenous Metabolite
|
Cancer
|
|
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 .
|
-
- HY-155556
-
|
|
ClpP
Biochemical Assay Reagents
|
Cancer
|
|
ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
|
-
- HY-120041
-
|
|
IRAK
|
Cancer
|
|
ND-2158 is a competitive IRAK4 inhibitor, with the Ki of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo .
|
-
- HY-156920
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
Cancer
|
|
VDX-111 is an analog of vitamin D. VDX-111 exhibits cytotoxicity in ovarian cancer cells through upregulation of RIPK1/RIPK3 pathway and induction of necroptosis. VDX-111 promotes expressions of cytokines and exhibits antitumor activity in mouse model .
|
-
- HY-149667
-
|
|
DGK
|
Cancer
|
|
BMS-332 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.005 (DGKα) and 0.001 μM (DGKζ) .
|
-
- HY-149666
-
|
|
DGK
|
Cancer
|
|
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.09 (DGKα) and 0.006 μM (DGKζ) .
|
-
- HY-157136
-
|
|
CRM1
COX
c-Myc
Survivin
|
Cancer
|
|
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
|
-
- HY-163006
-
|
|
EGFR
c-Met/HGFR
|
Cancer
|
|
EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
|
-
- HY-16160
-
|
|
Autophagy
ICMT
|
Cancer
|
|
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research .
|
-
- HY-163396
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
|
-
- HY-W010041
-
|
|
Amyloid-β
Endogenous Metabolite
|
Neurological Disease
|
|
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model .
|
-
- HY-148923
-
|
|
STAT
|
Cancer
|
|
MC0704 is a STAT3 inhibitor with an IC50 value of 2.13 μM. MC0704 induces cell apoptosis and cell cycle arrest. MC0704 shows antitumor activity in mouse breast cancer models. MC0704 can be used for the research of metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-P10019
-
|
NLY01
|
GCGR
|
Neurological Disease
|
|
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
|
-
- HY-146245C
-
|
CpG 1826 sodium
|
Toll-like Receptor (TLR)
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
ODN 1826 sodium is a class B CpG ODN (oligodeoxynucleotide) that is a TLR9 agonist. ODN 1826 sodium is an immunostimulatory agent that induces NO and iNOS production in mouse models. ODN 1826 sodium also enhances apoptosis (apoptosis) and may promote atherosclerosis. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’ .
|
-
- HY-157847
-
|
|
STAT
|
Cancer
|
|
Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
|
-
- HY-155740
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability .
|
-
- HY-N0421
-
|
Cinobufagine
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-120118
-
|
ML246
|
DNA/RNA Synthesis
|
Cancer
|
|
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-136181A
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- HY-136181
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models .
|
-
- HY-114196
-
|
ZGN-1061
|
MetAP
|
Metabolic Disease
|
|
Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells .
|
-
- HY-139915
-
|
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation .
|
-
- HY-145830
-
|
|
Adenylate Cyclase
|
Neurological Disease
|
|
AC1-IN-1 is a potent and selective Adenylyl cyclase type 1 (AC1) inhibitor with an IC50 of 0.54 µM. AC1-IN-1 displays modest antiallodynic effects in a mouse model of inflammatory pain. AC1-IN-1 has CNS activity .
|
-
- HY-P99604
-
|
AZD-1061; COV2-2130
|
SARS-CoV
|
Infection
|
|
Cilgavimab (AZD-1061; COV2-2130) is a human SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection .
|
-
- HY-148838
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research .
|
-
- HY-10834
-
|
|
β-catenin
|
Cancer
|
|
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway. β-catenin-IN-6 inhibits human colorectal cancer cells proliferation, as well as in a β-catenin/RK3E mouse model .
|
-
- HY-118594
-
|
|
Others
|
Metabolic Disease
|
|
Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate is a mouse-modeling drug that can induce Mallory body (MB) formation. MBs reached maximum concentration on day 5 of refeeding. Liver cell regeneration increased on the third day of refeeding .
|
-
- HY-155681
-
|
|
PD-1/PD-L1
Monoamine Oxidase
|
Cancer
|
|
SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%) .
|
-
- HY-162001
-
|
|
CDK
|
Cancer
|
|
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
|
-
- HY-163092
-
|
|
MAGL
Necroptosis
|
Inflammation/Immunology
|
|
LEI-515 is a first-in-class peripherally restricted, reversible MAGL inhibitor. LEI-515 increases 2-AG levels in peripheral organs, but not mouse brain. LEI-515 attenuated liver necrosis, oxidative stress and inflammation in a CCl4-induced acute liver injury model .
|
-
- HY-117356B
-
|
|
P2Y Receptor
NF-κB
ERK
|
Cardiovascular Disease
|
|
MRS2693 trisodium is a selective P2Y6 agonist with an EC50 value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model .
|
-
- HY-A0143A
-
|
DGLA sodium; all-cis-8,11,14-Eicosatrienoic acid sodium
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid (DGLA; all-cis-8,11,14-Eicosatrienoic acid) sodium is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid (sodium) attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- 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 .
|
-
- HY-148178
-
|
|
Parasite
|
Infection
|
|
MMV688533 is an antimalarial agent with rapid anti-plasmodial activity and effective single-dose activity against Plasmodium falciparum infection in humanized mouse models. MMV688533 can inhibit the activity of asexual blood stage parasites with an IC50 value of 1.3 nM. MMV688533 exhibits excellent pharmacokinetic properties and safety .
|
-
- HY-110216
-
|
|
CRAC Channel
|
Inflammation/Immunology
|
|
5J-4 is a potent CRAC inhibitor. 5J-4 decreases the numbers of infiltrated mononuclear cell into the CNS, and significantly decreases the population of infiltrated CD4+ population. 5J-4 reduces the symptoms and delayed the onset of EAE (experimental autoimmune encephalomyelitis) in mouse model of inflammation .
|
-
- HY-117985
-
|
DA-1229
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
Inflammation/Immunology
|
|
Evogliptin (DA-1229) is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-149950
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 106 (compound 10ic) is an anticancer agent that induces apoptosis in B16-F10 melanoma cells. Anticancer agent 106 also potently inhibits metastatic nodules in a mouse model of lung metastatic melanoma. Anticancer agent 106 can be used in the study of cancer, especially lung metastatic melanoma .
|
-
- HY-12768B
-
|
BLZ945 dihydrochloride
|
c-Fms
|
Neurological Disease
Cancer
|
|
Sotuletinib (BLZ945) dihydrochloride is an orally active and blood-brain barrier-permeable CSF1-R-specific inhibitor (IC50=1 nM). Sotuletinib (BLZ945) dihydrochloride induces tumor cell apoptosis and effectively inhibits tumor growth in mouse models. Sotuletinib dihydrochloride can be used in cancer and amyotrophic lateral sclerosis (ALS) research .
|
-
- HY-149631
-
|
|
HDAC
|
Cancer
|
|
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
|
-
- HY-B0702R
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline (Standard) is the analytical standard of Nicergoline. This product is intended for research and analytical applications. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease .
|
-
- HY-122664
-
|
|
BRK
|
Cancer
|
|
XMU-MP-2 is a BRK inhibitor with significant inhibitory activity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2 inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-163534
-
|
|
PD-1/PD-L1
|
Cancer
|
PD-1/PD-L1-IN-43 (compound Z13) is a small-molecule inhibitors targeting the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-43 exhibites potent in vivo antitumor efficacy against B16-F10 melanoma. PD-1/PD-L1-IN-43 inhibits tumor growth by blocking the interaction between PD-1 and PD-L1. PD-1/PD-L1-IN-43 can be used in anti-tumor studies .
|
-
- HY-122906
-
|
|
c-Fms
|
Inflammation/Immunology
|
|
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis .
|
-
- HY-123033A
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-123033
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-117985B
-
|
DA-1229 tartrate
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
Inflammation/Immunology
|
|
Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation .
|
-
- HY-154313
-
|
Clospirazine
|
Ras
|
Cancer
|
|
Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
|
-
- HY-149352
-
|
|
Thymidylate Synthase
|
Cancer
|
|
DG1 (Compound 8Nc) is a Thymidylate Synthase (TS) inhibitor that affects cancer angiogenesis and metabolic reprogramming in NSCLC cells. DG1 can effectively inhibit the expression of CD26, ET-1, FGF-1 and EGF. DG1 also effectively inhibits the proliferation of cancer tissue in the A549 xenograft mouse model .
|
-
- HY-149417
-
|
|
HDAC
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE/HDAC6-IN-1 is a potent and selective dual BChE/HDAC6 inhibitor with IC50 values of 4 and 8.9 nM, respectively. BChE/HDAC6-IN-1 ameliorates the cognitive impairment in an Aβ1–42-induced mouse model and has the potental for AD research .
|
-
- HY-160186
-
|
|
Others
|
Cardiovascular Disease
|
|
20-SOLA is the first water soluble and orally active 20-HETE antagonist. 20-SOLA greatly ameliorates changes in blood pressure and renal injury associated with a streptozotocin (STZ)-diabetic mouse model. 20-SOLA also is a GPR75 receptor blocker. 20-SOLA can be used for the research of cardiovascular pathologies .
|
-
- HY-N0109R
-
|
Rhodioloside (Standard)
|
Prolyl Endopeptidase (PREP)
mTOR
Apoptosis
PINK1/Parkin
|
Cancer
|
|
Salidroside (Standard) is the analytical standard of Salidroside. This product is intended for research and analytical applications. Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy .
|
-
- HY-162255
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer .
|
-
- HY-15079
-
|
GYKI-53773; LY-300164
|
iGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity . Talampanel (IVAX) has neuroprotective effects in rodent stroke models . Talampanel attenuates caspase-3 dependent apoptosis in mouse brain .
|
-
- HY-123522
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo .
|
-
- HY-114180
-
|
RU320521
|
Cyclic GMP-AMP Synthase
|
Metabolic Disease
|
|
RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS) .
|
-
- HY-12098
-
|
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-135953
-
|
|
Apoptosis
|
Cancer
|
|
CDDO-3P-Im is an analogue of CDDO-Imidazolide with chemopreventive effect. CDDO-3P-Im can reduce the size and the severity of the lung tumors in mouse lung cancer model . CDDO-3P-Im is a orally active necroptosis inhibitor that can be used for the research of ischemia/reperfusion (I/R) .
|
-
- HY-103370
-
|
BA 7602-06
|
Chloride Channel
|
Inflammation/Immunology
|
|
Talniflumate (BA 7602-06) is the proagent of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase . Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome .
|
-
- HY-W092043
-
-
- HY-139562
-
|
|
FXR
|
Metabolic Disease
|
|
BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
|
-
- HY-19345
-
|
NSC13316
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways . Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model . Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell .
|
-
- HY-B0702S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].
|
-
- HY-146086
-
|
|
Keap1-Nrf2
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
|
|
Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model .
|
-
- HY-19345A
-
|
NSC13316 dihydrochloride
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) dihydrochloride is a MKK4-specific activator that activates MAPK pathways . Vacquinol-1 dihydrochloride specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model . Vacquinol-1 dihydrochloride also induces apoptosis in hepatocellular carcinoma (HCC)cell .
|
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
|
-
- HY-155850
-
|
|
Pyruvate Kinase
|
Neurological Disease
|
|
CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction .
|
-
- HY-160061
-
|
|
Others
|
Cancer
|
|
P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
|
-
- HY-P10360
-
|
|
α-synuclein
|
Neurological Disease
|
|
Tat-βsyn-degron is an α-synuclein knockdown peptide. Tat-βsyn-degron binds toα-synuclein and reduces α-synuclein levels in primary rat cortical neuron cultures. Tat-βsyn-degron also reduces α-synuclein levels and decreases the parkinsonian toxin-induced neuronal damage and motor impairment in a mouse toxicity model of PD .
|
-
- HY-B0217
-
|
NTZ; NSC 697855
|
Parasite
Influenza Virus
Autophagy
|
Infection
Cancer
|
|
Nitazoxanide (NTZ), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans. Nitazoxanide inhibits Giardia lamblia trophozoite proliferation in axenic culture with an IC50 of 2.4 μM . Nitazoxanide can be used for the research of parasitic gastroenteritis. Nitazoxanide shows anti-Japanese encephalitis virus (JEV) activity in a mouse model .
|
-
- HY-122611
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
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-103171
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model .
|
-
- HY-136360
-
MI-3454
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
|
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .
|
-
- HY-123033B
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside tartrate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-123033C
-
|
|
Sirtuin
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Nicotinamide riboside malate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-143905
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- HY-143904
-
|
|
PROTACs
|
Cancer
|
|
PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells .
|
-
- 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-150639
-
|
|
Raf
|
Cancer
|
|
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
|
-
- HY-122611A
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
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
|
-
- HY-125065
-
|
|
Androgen Receptor
5 alpha Reductase
|
Endocrinology
Cancer
|
|
MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .
|
-
- HY-158148
-
|
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
|
|
CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC50 of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable .
|
-
- HY-161620
-
|
|
IRAK
|
Inflammation/Immunology
|
|
DW18134 is an inhibitor for interleukin receptor-associated kinase 4 (IRAK 4) with an IC50 of 11.2 nM. DW18134 inhibits phosphorylation of IRAK4 and IKK, downregulates the secretion of TNF-α and IL-6. DW18134 attenuates the Lipopolysaccharides (HY-D1056)-induced peritonitis and DSS-induced colitis in mouse models, and protects the intestinal barrier function .
|
-
- HY-146407
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity .
|
-
- HY-W115718
-
|
|
Dopamine β-hydroxylase
|
Neurological Disease
|
|
Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC) .
|
-
- HY-138131
-
|
|
Others
|
Neurological Disease
|
|
SOD1-Derlin-1 inhibitor-1 (compound 56-20) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-1 inhibits SOD1 G93A-Derlin-1 complex with an IC50 value of 7.11 μM. SOD1-Derlin-1 inhibitor-1 can be used for the research of amyotrophic lateral sclerosis .
|
-
- HY-123982
-
|
|
Others
|
Neurological Disease
|
|
SOD1-Derlin-1 inhibitor-2 (compound 56-59) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-2 attenuates the interactions between Derlin-1 and SOD1 mut. SOD1-Derlin-1 inhibitor-2 can be used for the research of amyotrophic lateral sclerosis (ALS) .
|
-
- HY-13954
-
|
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
|
-
- HY-14342
-
MK-5046
1 Publications Verification
|
Bombesin Receptor
|
Metabolic Disease
|
|
MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
|
-
- HY-138657
-
|
|
Phosphatase
|
Cancer
|
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model .
|
-
- HY-145245
-
-
- HY-150636
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
|
-
- HY-151462
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151933
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
|
-
- HY-148948
-
|
|
NAMPT
|
Neurological Disease
|
|
NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity .
|
-
- HY-N11499
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models .
|
-
- HY-155572
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator-8 (compound 10e) is a Nrf2 activator (EC50=37.9 nM). Nrf2 activator-8 exhibits remarkable antioxidant and anti-inflammatory effects in BV-2 microglial cells. Nrf2 activator-8 can significantly restore spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation .
|
-
- HY-153255
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-13 (Compound 36) is an orally active BACE1 inhibitor with an IC50 value of 2.9 nM. BACE1-IN-13 is highly potent in hAβ42 cell (IC50 = 1.3 nM). BACE1-IN-13 has cardiovascularly safty and elicits sustained Aβ42 reduction in mouse and dog animal models .
|
-
- HY-155971
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model .
|
-
- HY-N12044
-
|
|
Apoptosis
|
Cancer
|
|
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
|
-
- 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-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-157442
-
|
|
Salt-inducible Kinase (SIK)
|
Inflammation/Immunology
|
|
GLPG3312 (Compound 28) is a selective pan-SIK inhibitor with IC50 values of 2.0 nM, 0.7 nM and 0.6 nM for SIK1, SIK2 and SIK3, respectively. GLPG3312 exhibits anti-inflammatory and immunomodulatory activity in vitro on human primary myeloid cells and in vivo in mouse models. GLPG3312 has good oral bioavailability and can be used for research on inflammatory and immune diseases .
|
-
- HY-117049
-
|
|
CDK
DYRK
|
Neurological Disease
|
|
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) . Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model .
|
-
- HY-13440
-
AMG 511
2 Publications Verification
|
PI3K
|
Cancer
|
|
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
|
-
- HY-131328
-
|
LOXO-305
|
Btk
|
Cancer
|
|
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .
|
-
- HY-146462
-
|
|
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-47888
-
|
|
Integrin
|
Inflammation/Immunology
|
|
PLN-1474 (compound 1) is an orally active and selective ανβ1 integrin inhibitor with an IC50 value of <50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or researching a fibrotic or cirrhotic disease or disorder.
|
-
- HY-155532
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-128423AS
-
|
Acetylisovaleryltylosin-d9
|
Antibiotic
Bacterial
NF-κB
Apoptosis
Isotope-Labeled Compounds
|
Others
|
|
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9)is the deuterium labeledTylvalosin(HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
|
-
- HY-149426
-
|
|
Sirtuin
|
Inflammation/Immunology
|
|
SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .
|
-
- HY-157088
-
|
|
Caspase
Apoptosis
|
Others
|
|
C105SR is a cyclophilin D (CypD) inhibitor targeting to peptidyl-prolylcis-trans isomerase (PPIase). C105SR inhibits mitochondrial permeability transition opening (mPTP) with an IC 50 of 5 nM. C105SR inhibits hypoxia and reoxygenation inudced hepatocyte apoptosis and increases the level of calcium retention capacity (CRC). C105SR exhibits hepaprotective effect in ischaemia-reperfusion injury (IRI) mouse model .
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-
- HY-19443
-
|
|
Histamine Receptor
Lipoxygenase
|
Inflammation/Immunology
|
|
UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guinea pigs. UCB-35440 can be used for research on asthma and skin inflammation .
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-
- HY-162004
-
|
|
NF-κB
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model .
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-
- HY-162280
-
|
|
PROTACs
RANKL/RANK
Nuclear Factor of activated T Cells (NFAT)
Btk
|
Cancer
|
|
PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .
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-
- HY-15344
-
|
|
Others
|
Neurological Disease
Metabolic Disease
|
|
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
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-
- HY-19620
-
|
LMI070; NVS-SM1
|
DNA/RNA Synthesis
Potassium Channel
|
Cancer
|
|
Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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-
- HY-101855
-
|
Anle138b
|
Amyloid-β
|
Neurological Disease
|
|
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
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-
- HY-111751
-
|
|
iGluR
|
Neurological Disease
|
|
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models .
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-
- HY-15131
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
PNRI-299 is a selective AP-1 transcription inhibitor with an IC50 of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model .
|
-
- HY-110243
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
|
-
- HY-19620A
-
|
LMI070 hydrochloride; NVS-SM1 hydrochloride
|
DNA/RNA Synthesis
Potassium Channel
|
Cancer
|
|
Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
|
-
- HY-105395
-
|
|
Influenza Virus
|
Infection
|
|
BCX-1898, a cyclopentane derivative, is an orally active and selective influenza virus neuraminidase inhibitor. BCX-1898 has antiviral activity with EC50s of <0.01-21 μM on influenza A (H1N1, H3N2, and H5N1) and influenza B viruses replication in MDCK cells. BCX-1898 shows protection against the mouse influenza model .
|
-
- HY-149092
-
|
|
TAM Receptor
|
Cancer
|
|
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
|
-
- HY-156618
-
|
ABSK011
|
FGFR
|
Cancer
|
|
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
|
-
- HY-155993
-
|
|
PARP
|
Cancer
|
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
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-
- HY-163527
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50 = 0.20 ± 0.02 nM) and FGFR4(IC50 = 0.40 ± 0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-15186
-
Ipatasertib
Maximum Cited Publications
35 Publications Verification
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-17600
-
|
ACP-196
|
Btk
|
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 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P1416
-
|
|
Wnt
|
Cancer
|
|
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-A0143S
-
|
DGLA-d6; all-cis-8,11,14-Eicosatrienoic acid-d6
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
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-
- HY-112584
-
|
6-Methoxynicotinamide
|
Others
|
Metabolic Disease
|
|
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
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-
- HY-133012
-
|
|
TRP Channel
|
Neurological Disease
|
|
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
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-
- HY-136927
-
|
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STING
|
Inflammation/Immunology
Cancer
|
|
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
|
-
- HY-145253
-
|
|
PROTAC Linkers
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
|
-
- HY-145254
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
|
-
- HY-139602
-
|
|
Flavivirus
Dengue virus
Virus Protease
|
Infection
|
|
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
|
-
- HY-147008
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC) .
|
-
- HY-147935
-
|
|
Akt
|
Cancer
|
|
NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model .
|
-
- HY-143286
-
|
|
PROTACs
FLT3
|
Cancer
|
|
PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
|
-
- 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-117133
-
|
SF0166
|
Integrin
|
Metabolic Disease
|
|
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
|
-
- HY-W127408
-
|
|
Biochemical Assay Reagents
|
Others
|
|
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
|
-
- HY-156103
-
|
|
Huntingtin
|
Neurological Disease
|
|
mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitory activity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy .
|
-
- HY-155313
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC50 value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .
|
-
![β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE](//file.medchemexpress.com/product_pic/hy-155313.gif)
- HY-162011
-
|
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
GPR183 antagonist-2 (compound 32) is a selective GPR183 antagonist with good water solubility and excellent pharmacokinetic properties. GPR183 antagonist-2 significantly reduces paw and joint swelling and gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a collagen-induced arthritis (CIA) mouse model in a dose-dependent manner. GPR183 antagonist-2 can be used in the study of autoimmune diseases .
|
-
- HY-157317
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-126 (Compound II4) is a photoactive (IC50= 0.149) anticancer agent with significant near-infrared fluorescence emission at 650-760 nm. Antitumor agent-126 has antiproliferative activity and can induce apoptosis after laser irradiation. Antitumor agent-126 effectively inhibits tumor growth in mouse xenograft models exposed to 650 nm laser irradiation. Antitumor agent-126 can be used in cancer research .
|
-
- HY-139061
-
|
|
LPL Receptor
ROCK
|
Cancer
|
|
Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
|
-
- HY-107592
-
|
|
IKK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
|
-
- HY-158062
-
|
|
PROTACs
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research . (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
|
-
- HY-163538
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
|
-
- HY-155238
-
|
|
GABA Receptor
|
Neurological Disease
|
|
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
|
-
- HY-144643
-
|
|
Fungal
HDAC
Cytochrome P450
|
Inflammation/Immunology
|
|
CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis .
|
-
- HY-144126
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
|
-
- HY-150109
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia .
|
-
- HY-161383
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
|
-
- HY-16911
-
|
API-1252; Debio 1452
|
Bacterial
Antibiotic
|
Infection
|
|
AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ⩽0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
|
-
- HY-P1416A
-
|
|
Wnt
|
Cancer
|
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-110155
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .
|
-
- HY-138671
-
|
|
Bacterial
|
Infection
|
|
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
|
-
- HY-145255
-
|
|
PROTAC Linkers
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis .
|
-
- HY-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
|
-
- HY-124623
-
|
|
Parasite
|
Infection
|
|
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
|
-
- HY-147696
-
|
|
HSP
AMPK
Reactive Oxygen Species
|
Cancer
|
|
SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
|
-
- HY-143286A
-
|
|
PROTACs
FLT3
|
Cancer
|
|
PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader，with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells，can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
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-
- HY-153896
-
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|
c-Met/HGFR
|
Cancer
|
|
LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM .
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-
- HY-155780
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
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-
- HY-155195
-
|
|
Others
|
Cancer
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|
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
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-
- HY-149677
-
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|
Mitochondrial Metabolism
|
Cancer
|
|
ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
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-
- HY-100546
-
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|
Histone Demethylase
|
Infection
Metabolic Disease
Cancer
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|
GSK-LSD1 is a LSD1 inhibitor. GSK-LSD1 reduces food intake and body weight, and improves insulin sensitivity and glycemic control in mouse models of obesity. GSK-LSD1 also ameliorates NAFLD. GSK-LSD1 inhibits SARS-CoV-2-triggered cytokine release in COVID-19 PBMCs. GSK-LSD1 also inhibits cancer growth and metastasis .
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-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
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-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
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-
- HY-161072
-
|
|
NOD-like Receptor (NLR)
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Inflammation/Immunology
|
|
CSC-6 is a NLRP3 inhibitor. CSC-6 can significantly inhibit IL-1β secreted by PMATHP-1 cells with an IC50 value of 2.3 μM. CSC-6 specifically binds NLRP3 and inhibits NLRP3 activation by blocking ASC oligomerization during NLRP3 assembly. CSC-6 effectively reduces the symptoms of NLRP3 overactivation-mediated sepsis and gout in mouse models .
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-
- HY-161515
-
|
|
NAMPT
Epigenetic Reader Domain
|
Cancer
|
|
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
|
-
- HY-161520
-
|
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
|
Glucocorticoid receptor/NF-κB modulator-1 (Compound 20) is a derivative of ocotillol. Glucocorticoid receptor/NF-κB modulator-1 suppresses the degradation of glucocorticoid receptor (GR) mRNA and GR protein, inhibits the activation of NF-κB signaling pathway. Glucocorticoid receptor/NF-κB modulator-1 downregulates levels of NO, interleukin-6 and tumor necrosis factor-alpha (TNF-α). Glucocorticoid receptor/NF-κB modulator-1 ameliorates sepsis in mouse model .
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-
- HY-160912
-
|
|
ELOVL
|
Cancer
|
|
ELOVL6-IN-5 (compound B) is an inhibitor of the elongase enzyme of long-chain fatty acid family 6 (ELOVL6). ELOVL6 is a rate-limiting enzyme for the elongation of saturated and monounsaturated long-chain fatty acids and is an effective target for inhibiting diabetes. ELOVL6-IN-5 reduces hepatic fatty acid levels in a mouse model of diet-induced obesity (DIO). However, ELOVL6 inhibition by ELOVL6-IN-5 did not improve insulin resistance .
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-
- HY-132192
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model .
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-
- HY-111310
-
|
|
Lipoxygenase
|
Neurological Disease
Metabolic Disease
|
|
ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC50 of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2 . ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D .
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-
- HY-146755
-
|
|
Trk Receptor
|
Cancer
|
|
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
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-
- HY-132192A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model .
|
-
- HY-148813
-
|
|
PROTACs
STAT
|
Cancer
|
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-149948
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
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-
- HY-154851
-
|
|
GSK-3
CDK
Tau Protein
|
Neurological Disease
|
|
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
|
-
- HY-155781
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-155848
-
|
|
Phosphatase
|
Cancer
|
|
LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
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-
- HY-14342A
-
|
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Others
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Metabolic Disease
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|
(R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity .
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-
- HY-156025
-
|
|
Others
|
Inflammation/Immunology
|
|
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
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-
- HY-163481
-
|
|
Bacterial
|
Infection
|
|
Antibiofilm agent-6 (Compound 26c) is a quorum sensing inhibitor with strong antibiofilm effects that can inhibit the fluorescence intensity of PAO1-lasB-gfp and PAO1-pqsA-gfp in a concentration-dependent manner. Antibiofilm agent-6 can inhibit the production of pyocyanin and rhamnolipid. Antibiofilm agent-6 aids helps ciprofloxacin (HY-B0356) effectively eliminate the living bacteria in a mouse model infected with P. aeruginosa PAO1 .
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-
- HY-163512
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body. .
|
-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
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-
- HY-N10439
-
|
|
Glucosidase
|
Inflammation/Immunology
|
|
3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitory activity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibits MPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear .
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-
- HY-120920
-
|
|
Dopamine Receptor
|
Inflammation/Immunology
|
|
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .
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-
- 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-154968
-
|
|
RSV
|
Infection
|
|
RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection .
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-
- HY-115574
-
|
|
RSV
|
Infection
|
|
RSV L-protein-IN-1 (compound D) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.021 μM). RSV L-protein-IN-1 inhibits Polymerase (IC50=0.089 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-1 shows moderate cytotoxicity (CC50=8.4 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection .
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-157169
-
|
AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
|
-
- HY-163436
-
|
|
FXR
Cytochrome P450
RAR/RXR
PPAR
ROR
|
Metabolic Disease
|
|
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders .
|
-
- HY-33299
-
|
BTCA
|
Biochemical Assay Reagents
|
Cancer
|
|
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) .
|
-
- HY-163027
-
|
|
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research .
|
-
- HY-162065
-
|
|
Ferroptosis
|
Cancer
|
|
N6F11 is a ferroptosis inducer, and can trigger the degradation of glutathione peroxidase 4 (GPX4) specifically in cancer cells. N6F11 can be used for ferroptosis study .
|
-
- HY-149913
-
|
|
Others
|
Cancer
|
|
NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model .
|
-
- HY-155523
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
|
Cancer
|
|
Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
|
-
- HY-155731
-
|
|
Influenza Virus
|
Infection
|
|
Antiviral agent 35 (compound 4d) is an orally active and potent influenza virus inhibitor, acting function in the early stage of virus replication. Antiviral agent 35 inhibits ROS accumulation, autophagy and apoptosis induced by influenza virus, and also inhibits inflammatory response mediated by RIG-1 pathway in mouse model with pulmonary infection. Antiviral agent 35 shows little cytotoxicity with CC50 >800 μM in MDCK cells, and anti-H1N1 (A/Weiss/43) activity with EC50 of 2.28 μM .
|
-
- HY-155732
-
|
|
Parasite
|
Infection
|
|
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
|
-
- HY-149543
-
|
|
Mitochondrial Metabolism
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
|
BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells .
|
-
- HY-161023
-
|
|
Others
|
Cancer
|
|
Importin β1-IN-1 (compound DD1-Br) is an orally active Importin β1 inhibitor (KD = 0.219 μM). Importin β1-IN-1 exhibits antiproliferative activity on castration-resistant prostate cancer (CRPC) cells. Importin β1-IN-1 alone or in combination with enzalutamide completely prevented tumor growth in a mouse model of drug-resistant CRPC. Importin β1-IN-1 can be used in cancer research .
|
-
- HY-123960A
-
|
|
Phosphatase
|
Neurological Disease
|
|
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 .
|
-
- HY-123960
-
|
|
Phosphatase
|
Neurological Disease
|
|
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 .
|
-
- HY-148409
-
|
|
Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
|
-
- HY-113058
-
|
|
Biochemical Assay Reagents
|
Others
|
|
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
|
-
- HY-143881
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-144088
-
|
HPK1-IN-22
|
MAP4K
|
Inflammation/Immunology
Cancer
|
|
ZYF0033 is effective in inhibiting hematopoietic progenitor cells HPK1, basically inhibiting MBP protein oxidation IC50 10 nM . ZYF0033 promotes anti-cancer immune response, lowers SLP76 (acid 376) oxidation. ZYF0033 Suppression 4T-1 Small mouse model with the same underlying cause, medium bulge growth length expansion DC, NK 细细和 CD107a + CD8 + T Cells, PD-1 +CD8 + T Cells, TIM-3 +CD8 + T Cells LAG3< sup>+CD8 + T Cellular immersion decreases.
|
-
- HY-124832
-
|
|
Caspase
Amyloid-β
|
Neurological Disease
|
|
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
|
-
- HY-150613
-
|
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-161615
-
|
|
Apoptosis
PROTACs
|
Cancer
|
|
PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
|
-
- HY-115987
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
|
-
- HY-150609
-
|
|
SHP2
Phosphatase
CDK
|
Cancer
|
|
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-151411
-
|
|
Others
|
Cancer
|
|
RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model .
|
-
- HY-156110
-
|
|
Insulin Receptor
|
Cancer
|
|
IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
|
-
- HY-156296
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .
|
-
- HY-129602
-
SD-36
5 Publications Verification
|
PROTACs
STAT
Apoptosis
|
Cancer
|
|
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-156096
-
|
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
|
-
- 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 .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-114360A
-
|
|
Biochemical Assay Reagents
|
|
Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model.
|
-
- HY-113058
-
|
|
Biochemical Assay Reagents
|
|
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
|
-
- HY-131420
-
|
Aseanostatin P1; Isotetradecanoic acid
|
Biochemical Assay Reagents
|
|
12-Methyltridecanoic acid is a methylated fatty acid that has been found in milk. 12-Methyltridecanoic acid (200 μM) reduces angiogenesis and corneal opacity in alkaline or Pseudomonas aeruginosa-induced ocular mouse models.
|
-
- HY-W127408
-
|
|
Biochemical Assay Reagents
|
|
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-156430
-
|
|
MMP
|
Cancer
|
|
MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction .
|
-
- HY-145237
-
|
|
Peptides
|
Cancer
|
|
BM213, a potent and selective agonist for C5aR1, shows antitumor activity in a mouse model of mammary carcinoma.
|
-
- HY-P4253
-
|
|
VEGFR
|
Cardiovascular Disease
|
|
Arginyl-Glutamine is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy .
|
-
- HY-P5183
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Hm1a is a disulfide-rich spider-venom peptide, and a NaV1.1 activator. Hm1a restores the function of inhibitory interneurons in Dravet syndrome (DS) mouse model .
|
-
- HY-P3350
-
|
|
Bacterial
|
Infection
|
|
LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
|
-
- HY-P2464
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Myosin H Chain Fragment, mouse is a fragment of the α-Myosin heavy chain peptide. Myosin H Chain Fragment can be used to induce experimental autoimmune myocarditis (EAM) mouse model .
|
-
- HY-P2464A
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Myosin H Chain Fragment, mouse acetate salt is a fragment of the α-Myosin heavy chain peptide. Myosin H Chain Fragment can be used to induce experimental autoimmune myocarditis (EAM) mouse model .
|
-
- HY-P1727
-
|
|
YAP
|
Cancer
|
|
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P1727A
-
|
|
YAP
|
Cancer
|
|
Super-TDU TFA is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU TFA suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P2287
-
|
|
CRFR
|
Neurological Disease
|
|
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an EC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive agent in the mouse model .
|
-
- HY-P1787
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (4-10) is an epitope for the polyclonal anti-Aβ(1-42) antibody, reduces amyloid deposition in a transgenic Alzheimer disease mouse model .
|
-
- HY-P4866
-
|
|
Peptides
|
Metabolic Disease
|
|
Q-Peptide is the angiopoietin-1 derived peptide (QHREDGS).Q-Peptide increases keratinocyte migration to improve wound healing, in diabetic mouse model. Q-Peptide accelerates wound closure .
|
-
- HY-P3341
-
-
- HY-P5907
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-P1728
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) is a peptide fragment of Super-TDU. Super-TDU (1-31) is an inhibitor of YAP-TEAD complex. Super-TDU shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P1728A
-
|
|
YAP
|
Cancer
|
|
Super-TDU (1-31) TFA is a peptide fragment of Super-TDU. Super-TDU (1-31) TFA is an inhibitor of YAP-TEAD complex. Super-TDU TFA shows potent anti-tumor activity and suppresses tumor growth in gastric cancer mouse model .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613)
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-P10019
-
|
NLY01
|
GCGR
|
Neurological Disease
|
|
Pegsebrenatide (NLY01) is a long-acting GLP-1R agonist. Pegsebrenatide has an extended half-life and favorable blood-brain barrier penetration. Pegsebrenatide can block A1 astrocyte transformation, reducing dopaminergic cell death, and improving motor symptoms in mouse models of PD .
|
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
|
-
- HY-P10360
-
|
|
α-synuclein
|
Neurological Disease
|
|
Tat-βsyn-degron is an α-synuclein knockdown peptide. Tat-βsyn-degron binds toα-synuclein and reduces α-synuclein levels in primary rat cortical neuron cultures. Tat-βsyn-degron also reduces α-synuclein levels and decreases the parkinsonian toxin-induced neuronal damage and motor impairment in a mouse toxicity model of PD .
|
-
- HY-163001
-
|
|
Autophagy
p62
Atg8/LC3
|
Cancer
|
|
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
|
-
- HY-P1416
-
|
|
Wnt
|
Cancer
|
|
Foxy-5, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-P10376
-
|
|
Peptides
|
Cancer
|
|
Lucicebtide (Compound ST101) is a selective antagonist for CCAAT/enhancer binding protein β (C/EBPβ). Lucicebtide binds to the leucine zipper domain of C/EBPβ, prevents its dimerization, and ubiquitin-dependently degrades C/EBPβ. Lucicebtide arrests cell cycle at G0/G1 phase. Lucicebtide exhibits cytotoxicity in cancer cells. Lucicebtide exhibits good pharmacokinetic characters and inhibits tumor growth in mouse model .
|
-
- HY-P1416A
-
|
|
Wnt
|
Cancer
|
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model .
|
-
- HY-P5396
-
|
|
Peptides
|
Others
|
|
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
|
-
- HY-K6008
-
|
|
|
MCE Basement Membrane Matrix HC is primarily composed of natural basement membrane matrix extracted from mouse tumors, with higher content of various cytokines than the standard type.This product is mainly used for angiogenesis experiments, construction of animal models and 3D tumor models.
|
-
- HY-K6005
-
|
|
|
MCE Basement Membrane Matrix HC (Phenol Red) is primarily composed of natural basement membrane matrix extracted from mouse tumors, with higher content of various cytokines than the standard type.This product is mainly used for angiogenesis experiments, construction of animal models and 3D tumor models.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99590A
-
|
|
Inhibitory Antibodies
|
Cardiovascular Disease
|
|
Sotatercept (mIgG2a) has direct cardioprotective actions, which reduces right ventricular (RV) remodeling and improves function in a pulmonary artery banding (PAB) mouse model .
|
-
- HY-P99351
-
|
Anti-MMP9 Reference Antibody (andecaliximab)
|
MMP
|
Cancer
|
|
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-P99604
-
|
AZD-1061; COV2-2130
|
SARS-CoV
|
Infection
|
|
Cilgavimab (AZD-1061; COV2-2130) is a human SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection .
|
-
- HY-P99578
-
|
HL036337; HBM9036
|
TNF Receptor
|
Others
|
|
Tanfanercept (HL036337) is an anti-TNF-α monoclonal antibody. Tanfanercept is effective in ameliorating corneal erosions in a dry eye (DE) mouse model .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- 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-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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B1899S
-
|
|
|
Taurodeoxycholic acid-d5is the deuterium labeledTaurodeoxycholic acid(HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
|
-
-
- HY-126242S
-
|
|
|
Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].
|
-
-
- HY-157029S
-
|
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-157031S
-
|
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
-
- HY-B0149S3
-
|
|
|
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
|
-
-
- HY-B0702S
-
|
|
|
Nicergoline- 13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease[1][2].
|
-
-
- HY-W757743
-
|
|
|
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-128423AS
-
|
|
|
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9)is the deuterium labeledTylvalosin(HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
|
-
-
- HY-A0143S
-
|
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157029S
-
|
|
|
Alkynes
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
|
Alkynes
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
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