Search Result
Results for "
Inhibitor
" in MedChemExpress (MCE) Product Catalog:
9935
Inhibitors & Agonists
14
Biochemical Assay Reagents
147
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-16695
-
|
Inhibitor of Mcl-1
|
Bcl-2 Family
|
Cancer
|
|
MIM-1 is an inhibitor of myeloid cell factor 1 (Mcl-1).
|
-
- HY-131005
-
-
- HY-156781
-
|
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Sirtuin
|
Metabolic Disease
|
|
Sirtuin-1 inhibitor 1 (Compound 8) is an inhibitor of Sirtuin-1 that plays important roles in obesity-induced diabetes and aging-related diseases.
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-
- HY-14412
-
|
|
p38 MAPK
|
Cancer
|
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p38α inhibitor 4 (compound 10) is a selective and allosteric p38α inhibitor with an IC50 value of 1.2 μM. p38α inhibitor 4 exhibits no activity against p38β, p38γ, and p38δ.
|
-
- HY-146709
-
-
- HY-P10066
-
-
- HY-145826
-
|
|
Bcl-2 Family
|
Cancer
|
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Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112.
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-
- HY-156819
-
|
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Others
|
Others
|
|
KRAS G12D inhibitor 18 is a potent KRAS G12D inhibitor.
|
-
- 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-113571
-
|
|
Tie
|
Cardiovascular Disease
|
|
Tie2 kinase inhibitor 2 (compound 7) is a selective Tie2 kinase inhibitor with an IC50 value of 1 μM. Tie2 kinase inhibitor 2 inhibits endothelial cell tube formation, and can be used for Tie2-mediated angiogenic disorders research.
|
-
- HY-157166
-
|
|
EGFR
|
Cancer
|
|
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer.
|
-
- HY-149636
-
|
|
VEGFR
CDK
EGFR
|
Cancer
|
|
Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
|
-
- HY-149725
-
|
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MMP
|
Neurological Disease
|
proMMP-9 selective inhibitor-1 (compound 33) is a highly potent and selective inhibitor of proMMP-9 activation.
|
-
- HY-142934
-
|
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ROR
|
Inflammation/Immunology
Cancer
|
|
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC50 of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt.
|
-
- HY-119374
-
|
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Epigenetic Reader Domain
|
Cancer
|
|
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.
|
-
- HY-142853
-
|
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Carbonic Anhydrase
|
Endocrinology
|
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Carbonic anhydrase inhibitor 3 (compound 11g) is a carbonic anhydrase II inhibitor. Carbonic anhydrase inhibitor 3 reduces the intraocular pressure in glaucomatous rabbits.
|
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- HY-142849
-
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Carbonic Anhydrase
|
Endocrinology
|
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Carbonic anhydrase inhibitor 1 (compound 7c) is a carbonic anhydrase II inhibitor. Carbonic anhydrase inhibitor 3 reduces the intraocular pressure in glaucomatous rabbits.
|
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- HY-142460
-
|
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Ras
|
Cancer
|
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KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1).
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- HY-142458
-
|
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Ras
|
Cancer
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KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737).
|
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- HY-142457
-
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Ras
|
Cancer
|
|
KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737).
|
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- HY-P5989
-
|
Mu-Val-HPh-FMK
|
Antibiotic
|
Infection
|
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Calpain inhibitor V (Mu-Val-HPh-FMK) is a cell-permeable and irreversible inhibitor of calpain that has anti-chlamydial activity.
|
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- HY-115880
-
|
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Ras
|
Cancer
|
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KRAS G12D inhibitor 3 is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 has antitumor effects (WO2022002102A1; compound 146). KRAS G12D inhibitor 3 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-118933
-
|
SJA6017
|
Proteasome
|
Others
|
|
Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.
|
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- HY-112546
-
|
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MMP
|
Cancer
|
|
MMP-2 Inhibitor I (OA-Hy) is a potent MMP-2 inhibitor with a Ki of 1.7 μM.
|
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- HY-115880A
-
|
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Ras
|
Cancer
|
|
KRAS G12D inhibitor 3 TFA is a KRAS G12D inhibitor with an IC50 of <500 nM. KRAS G12D inhibitor 3 TFA has antitumor effects (WO2022002102A1; compound 146). KRAS G12D inhibitor 3 (TFA) 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-146739
-
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Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research.
|
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- HY-152156
-
|
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
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Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.
|
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- HY-154986
-
|
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AMPK
|
Cancer
|
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MARK4 inhibitor 2 is an inhibitor of microtubule affinity-regulating kinase 4 (MARK4) with an Km of 6.3×10 7 and an IC50 of 0.82 μM. MARK4 inhibitor 2 inhibits the growth of human cells and can be used for cancer research.
|
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- HY-147705
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects.
|
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- HY-149524
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 8 (compound 10) is a competitive inhibitor (IC50: 5.38 μM) of sirtuin SIRT5 with anticancer potential.
|
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- HY-149525
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 9 (compound 14) is a competitive inhibitor (IC50: 4.07 μM) of sirtuin SIRT5 with anticancer potential.
|
-
- HY-149350
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT.
|
-
- HY-149694
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora Kinase Inhibitor-12 (Compound 1a ) is the inhibitor of aurora kinase which is a key enzyme that is implicated in tumor growth.
|
-
- HY-142467
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-11, a fused pyridine ring derivative, is a HIV-1 inhibitor. WO2021104413A1 ( compound 1-1b).
|
-
- HY-112412
-
|
PDGF Receptor Tyrosine Kinase Inhibitor III
|
PDGFR
|
Neurological Disease
|
|
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis.
|
-
- HY-119423
-
|
|
MMP
|
Cancer
|
|
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively.
|
-
- HY-115999
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.
|
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- HY-149856
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research.
|
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- HY-155138
-
|
|
Glutaminase
|
Cancer
Metabolic Disease
|
|
GLS1 Inhibitor-7 (compound 4d) is a GLS1 inhibitor (IC50=46.7 μM), with potential anti-cancer, anti-aging and anti-obesity properties.
|
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- HY-155090
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity.
|
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- HY-103271
-
|
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Bcl-2 Family
|
Cancer
|
|
Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro.
|
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- HY-155029
-
|
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Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-16 is a soluble epoxide hydrolase (sEH) inhibitors with an IC50 of 2 nM. sEH inhibitor-16 reduces the inflammatory damage in Cerulein (HY-A0190)-induced acute pancreatitis (AP) in mice and can be used for inflammation/immunology research.
|
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- HY-154852
-
|
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GSK-3
CDK
|
Neurological Disease
|
|
GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies.
|
-
- HY-143280
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
|
-
- HY-149018
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) with IC50 of 218 nM but lost its inhibitory activity of LPAR1.
|
-
- HY-P10072
-
|
Hsp25 kinase Inhibitor; Mk2 pseudosubstrate
|
ERK
JNK
p38 MAPK
HSP
MAPKAPK2 (MK2)
|
Others
|
|
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation.
|
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- HY-143235
-
|
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research.
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- HY-143402
-
|
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Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer.
|
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- HY-143721
-
|
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Monoamine Oxidase
|
Metabolic Disease
Cardiovascular Disease
Inflammation/Immunology
|
|
SSAO inhibitor-2 (Compound 1) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 10-100 μM for human SSAO and MAO-A, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
|
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- HY-143723
-
|
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Monoamine Oxidase
|
Metabolic Disease
Cardiovascular Disease
Inflammation/Immunology
|
|
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
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- HY-157039
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1/3-IN-1 (Compound 10) is a RIPK1 and RIPK3 inhibitor. RIPK1/3-IN-1 specifically inhibits necroptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation.
|
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- HY-N12405
-
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Calmodulin
|
Others
|
|
Encecalinol, extracted from aerial parts of Ageratina grandifolia, is a potent inhibitor of calmodulin inhibitor.
|
-
- HY-149718
-
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HDAC
JAK
|
Cancer
|
|
Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models.
|
-
- HY-156373
-
|
|
Others
|
Others
|
|
MN714 is a pivaloyloxymethyl (POM) protected inhibitor.
|
-
- HY-148249
-
|
|
MALT1
|
Cancer
|
|
NVS-MALT1 is a MALT1 allosteric inhibitor.
|
-
- HY-116238
-
|
|
ROCK
|
Others
|
|
ROCK-IN-D2 is a potent and selective ROCK inhibitor.
|
-
- HY-10250
-
|
TCN-P
|
ATP Synthase
|
Metabolic Disease
|
|
Triciribine phosphate (TCN-P) inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity.
|
-
- HY-117194
-
|
|
HIV
GSK-3
|
Infection
|
|
18BIOder is a neuroprotective GSK-3β inhibitor, highly selectively inhibiting HIV-1.
|
-
- HY-70005
-
|
Carboxypeptidase Inhibitor
|
Carboxypeptidase
|
Metabolic Disease
|
|
CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a Ki of 0.32 μM.
|
-
- HY-118525
-
|
|
HCV
PI4K
|
Infection
|
|
AL-9 is a inhibitor of PI4KIIIα, with the IC50 of 0.57 μM, that can inhibit HCV replication.
|
-
- HY-157130
-
|
|
Bacterial
|
Infection
|
T3SS-IN-3 (compound F-24) is an inhibitor of type III secretion system (T3SS). T3SS-IN-3 inhibits the transcription of hrpY gene significantly without inhibiting bacterial growth.
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-
- HY-107622
-
|
|
Others
|
Metabolic Disease
|
|
(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
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- HY-49066
-
-
- HY-157122
-
|
|
Others
|
Cancer
|
|
VJDT is a TREM1 small molecule inhibitor that effectively blocks TREM1 signaling. VJDT inhibits tumor growth and can be used in cancer research.
|
-
- HY-136123
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
|
-
- HY-136122
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
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-
- HY-136121
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
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- HY-155482
-
|
|
Others
|
Neurological Disease
|
|
NA-184 is a selective calpain-2 inhibitor. NA-184 inhibits TBI-induced cell death with an EC50 of 0.13 mg/kg.
|
-
- HY-151996
-
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|
Microtubule/Tubulin
|
Cardiovascular Disease
|
|
Tubulin inhibitor 31 is a potent tubulin inhibitor with an IC50 value of 4 µM. Tubulin inhibitor 31 shows anti-proliferative activity. Tubulin inhibitor 31 inhibits the HUVEC migration.
|
-
- HY-157148
-
|
|
Trk Receptor
c-Met/HGFR
|
Cancer
|
|
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors.
|
-
- HY-122874
-
-
- HY-149665
-
|
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DGK
|
Cancer
|
|
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes.
|
-
- HY-157145
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-69 (Compound 7E) is a non-covalent SARS-CoV-2 inhibitor with an EC50 value of 7.4 μM. SARS-CoV-2-IN-69 is a potent inhibitor of SARS-CoV-2 main protease (M pro) and a non-covalent inhibitor of papain (PL pro).
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-
- HY-147891
-
|
|
Apoptosis
|
Cancer
|
|
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos.
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-
- HY-147890
-
|
|
Apoptosis
|
Cancer
|
|
Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos.
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-
- HY-34386
-
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PARP
|
Cancer
Inflammation/Immunology
|
|
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research.
|
-
- HY-156554
-
|
|
Raf
|
Cancer
|
|
Raf inhibitor 3 (Example 30) is a Raf inhibitor. Raf inhibitor 3 inhibits B-Raf and C-Raf with IC50 values less than 15 nM. Raf inhibitor 3 can be used for research of cancers.
|
-
- HY-146711
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity.
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity.
|
-
- HY-145821
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 15 is a potent tubulin inhibitor. Tubulin inhibitor 15 shows antiproliferative activity. Tubulin inhibitor 15 shows cytotoxicity in HepG2 cells.
|
-
- HY-145822
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 16 is a potent tubulin inhibitor. Tubulin inhibitor 16 shows antiproliferative activity. Tubulin inhibitor 16 shows cytotoxicity in HepG2 cells.
|
-
- HY-128403
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM.
|
-
- HY-P5793
-
-
- HY-115956
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases.
|
-
- HY-144818
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia.
|
-
- HY-W404002
-
|
|
Prolyl Endopeptidase (PREP)
|
Metabolic Disease
|
|
BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
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-
- HY-153159
-
|
|
Others
|
Cancer
|
|
Angiogenesis inhibitor 4 is a potent angiogenesis inhibitor. Angiogenesis inhibitor 4 can be used in research of cancer.
|
-
- HY-115957
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 19 (compound 9b) is a potent inhibitor of tubulin. Tubulin inhibitor 19 is an indole chalcone compound. Tubulin inhibitor 19 has the potential for the research of cancer diseases.
|
-
- HY-145828
-
|
|
Microtubule/Tubulin
Ferroptosis
|
Cancer
|
|
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
|
-
- HY-P5988
-
|
|
PKC
|
Cancer
|
|
N-myristoyl-RKRTLRRL inhibits binding of PKC substrates. N-myristoyl-RKRTLRRL inhibits Ca 2+- and phosphatidylserine (PS)-dependent histone phosphorylation with IC50 of 5 μM.? histone phosphorylation with IC50 of 80 μM.
|
-
- HY-151983
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant.
|
-
- HY-114199
-
-
- HY-153692
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 1 (example 7) is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity. WRN inhibitor 1 has the potential to study cancer.
|
-
- HY-115958
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 20 (compound 1) is a potent inhibitor of tubulin. Tubulin inhibitor 20 has the potential for the research of cancer diseases.
|
-
- HY-147888
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site.
|
-
- HY-144766
-
|
|
Apoptosis
|
Cancer
|
|
ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation.
|
-
- HY-128617
-
|
|
Legumain
|
Cancer
|
|
Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
|
-
- HY-P5179
-
|
HWTX-I
|
Sodium Channel
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively.
|
-
- HY-143420
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model.
|
-
- HY-145820
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 14 is a potent NQO2 (quinone oxidoreductase 2) inhibitor with an IC50 of 1.0 μM. Tubulin inhibitor 14 also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule-destabilizing agent with potential tumor-selectivity and antiangiogenic and vascular disrupting features.
|
-
- HY-143251
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 13 (E27) is a potent tubulin inhibitor with an IC50 value of 16.1 μM for the tubulin polymerization inhibition. Tubulin inhibitor 13 inhibits migration and invasion of cancer cells, induces apoptosis and has anticancer activity.
|
-
- HY-112607
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-N3464
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity.
|
-
- HY-151879
-
-
- HY-147726
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability.
|
-
- HY-146205
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis.
|
-
- HY-146672
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.
|
-
- HY-147727
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization.
|
-
- HY-142644
-
-
- HY-157146
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-23 (Compound 15C) is an inhibitor of heme-mediated induction of the NLRP3 inflammasome. NLRP3-IN-23 significantly inhibits heme-mediated induction of the NLRP3 inflammasome at a concentration of 0.1 μM.
|
-
- HY-132196
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.
|
-
- HY-P5995
-
|
|
Elastase
|
Cancer
|
|
MeOSuc-AAPA-CMK is a potent inhibitor of human neutrophil elastase.
|
-
- HY-153594
-
-
- HY-149364
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 34 (compound b5) is a potent anticancer agent. Tubulin inhibitor 34 can inhibit tubulin polymerization and induce G2/M arrest and apoptosis. Tubulin inhibitor 34 exhibits significant antivascular and antitumor activity.
|
-
- HY-155342
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
A3373, a novel chemical inhibitor of Phospholipase D1 (PLD1) and PLD2, with IC50 of 325 nM and 15.15?μM, respectively, inhibits LPS-induced immune response and plays important roles in autoimmune arthritis, bone demineralization and osteoclastogenesis.
|
-
- HY-152150
-
|
|
Others
|
Metabolic Disease
|
|
Thrombin inhibitor 7 is a potent FXIIa inhibitor with IC50 values of 28 nM, >132 µM for FXIIa and FXIa, respectively. Thrombin inhibitor 7 shows low cytotoxicity.
|
-
- HY-131705
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.
|
-
- HY-10217
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2.
Thrombin Inhibitor 2 has antithrombotic activity.
|
-
- 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-149375
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 37 (Compound 12) is a Tubulin inhibitor that can effectively inhibit Tubulin aggregation (IC50=1.3 µM). Tubulin inhibitor 37 exhibits antiproliferative activity against human tumor cell lines and has potential for studying cancer.
|
-
- HY-P10117
-
-
- HY-144817
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 27 (DYT-1) is a tubulin polymerisation inhibitor with an IC50 of 25.6 µM. Tubulin inhibitor 27 shows anti-angiogenesis and antitumor activities.
|
-
- HY-146889
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 µM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells.
|
-
- HY-146890
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 µM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells.
|
-
- HY-139881
-
|
|
Btk
|
Cancer
|
|
BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
|
-
- HY-143730
-
|
|
Btk
|
Cancer
|
|
BTK inhibitor 20 is a potent BTK inhibitor with an IC50 of 8 nM.
|
-
- HY-142296
-
-
- HY-157151
-
|
|
Histone Methyltransferase
|
Cancer
|
|
iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively.
|
-
- HY-144748
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 17 (Compound 3b) is a tubulin polymerization inhibitor with an IC50 of 12.38 µM. Tubulin inhibitor 17 has anticancer activities and induces cell apoptosis.
|
-
- HY-15358
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
|
-
- HY-15357
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
|
-
- HY-152214
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor.
|
-
- HY-153692A
-
|
|
Biochemical Assay Reagents
|
Others
|
|
(R)-WRN inhibitor 1 is the R-isomer of WRN inhibitor 1 (example 7). WRN inhibitor 1 is a WRN inhibitor with anticancer activity.
|
-
- HY-153745
-
|
|
Trk Receptor
|
Cancer
|
|
Protein kinase inhibitor 5 is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 inhibits cell viability.
|
-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight.
|
-
- HY-146778
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis.
|
-
- HY-156579
-
|
|
Others
|
Cancer
|
|
WRN inhibitor 3 (example 110), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 3 can be used for the research of cancer.
|
-
- HY-143250
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity.
|
-
- HY-156580
-
|
|
Others
|
Cancer
|
|
WRN inhibitor 4 (example 107), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 4 can be used for the research of cancer.
|
-
- HY-156581
-
|
|
Others
|
Cancer
|
|
WRN inhibitor 5 (example 157), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 5 can be used for the research of cancer.
|
-
- HY-13278A
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.
|
-
- HY-124638
-
|
|
MNK
|
Cancer
|
|
MNK inhibitor 9 is a potent and selective inhibitor of MNK1/2 with IC50 values of 0.003 µM and 0.003 µM for MNK1 and MNK2 respectively. MNK inhibitor 9 has good cell permeability. MNK inhibitor 9 can be used in tumor related research.
|
-
- HY-149374
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 36 (Compound 10) is a novel and potent tubulin inhibitor and inhibits the polymerization of microtubular protein then induces apoptosis with an IC50 value of 1.5±0.1 μM. Tubulin inhibitor 36 (Compound 10) has significant anti-mitotic effect and exhibits activities against glioblastoma cells. Tubulin inhibitor 36 (Compound 10) has anti-tumor effects and can be used for glioblastoma multiforme (GBM) research.
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model.
|
-
- HY-W013478
-
|
|
Phosphatase
|
Cancer
|
|
PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect.
|
-
- HY-112913
-
-
- HY-13276
-
-
- 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-156130
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. Menin-MLL inhibitor 29 binds to Menin with a KD value of 138 nM, and inhibits the binding of Menin to MBM1 (Menin-binding motif 1) with an IC50 value of 46 nM. Menin-MLL inhibitor 29 inhibits HepG2 and Hep3B hepatoma cell proliferation (IC50s: 0.31 μM and 0.71 μM). Menin-MLL inhibitor 29 inhibits tumor growth.
|
-
- HY-125997
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
|
-
- HY-148037
-
|
|
Proteasome
|
Cardiovascular Disease
|
|
Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism.
|
-
- HY-147887
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells.
|
-
- HY-P4030
-
|
|
HIV Protease
|
Infection
|
|
Herpes virus inhibitor 2 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 2 inhibits viral replication.
|
-
- HY-P4028
-
|
|
Virus Protease
|
Infection
|
|
Herpes virus inhibitor 1 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 1 inhibits viral replication.
|
-
- HY-157254
-
|
|
Glutaminase
|
Cancer
|
|
AA10 is a potent and irreversible transglutaminase 2 (TG2) inhibitor for cancer research.
|
-
- HY-144647
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SP inhibitor 1 (compound 34) is a selective SARS-CoV-2 spike protein (SP) inhibitor with an IC50 of 3.26 μM, >25 μM, >25 μM for SP, M pro and PL pro protein, respectively. SP inhibitor 1 is a vitro SARS-CoV-2 replication inhibitor at non-toxic concentrations (0.3250<5.98 μM). SP inhibitor 1 shows cellular antiviral activity.
|
-
- HY-147725
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization.
|
-
- HY-143237
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research.
|
-
- HY-10439
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-143419
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 14 (compound 4), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 0.41 nM. ATX inhibitor 14 has the potential for fibrosis relevant diseases research.
|
-
- HY-154987
-
|
|
Others
|
Cancer
|
|
MAPK4 inhibitor 3 (compound 23b) is an inhibitor of MAPK4 with an IC50 value of 1.01 μM. MAPK4 inhibitor 3 inhibits cancer cells growth. MAPK4 inhibitor 3 can be used for research on cancer and tauopathies.
|
-
- HY-146122
-
-
- HY-146124
-
-
- HY-124793A
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.
|
-
- HY-124793
-
|
|
Cyclin G-associated Kinase (GAK)
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
|
-
- HY-157225
-
|
|
α-synuclein
|
Metabolic Disease
|
|
Brazilin-7-acetate (B-7-A) is an inhibitor of α-synuclein (α-Syn) aggregates. Brazilin-7-acetate inhibits the formation of α-synuclein fibril, mitigates cytotoxicity, and decreases oxidative stress. Brazilin-7-acetate can be used in the research of Parkinson's disease.
|
-
- HY-143583
-
|
|
Others
|
Cancer
Neurological Disease
|
|
ATX inhibitor 10 is a potent inhibitor of ATX. ATX inhibitor 10 is s nitrogen-containing heterocyclic compound. ATX plays a role in causing pathological conditions including fibrosis, arthritis, neurodegeneration, neuropathic pain, and cancer. ATX inhibitor 10 has the potential for the research of ATX related diseases (extracted from patent WO2021115375A1, compound 35).
|
-
- HY-121213
-
|
|
Cytochrome P450
|
Cancer
|
|
Erysolin is a CYP1A inhibitor with antigenic toxicity. Erysolin reduces benzo(a)pyrene-induced genotoxicity.
|
-
- HY-156013
-
-
- HY-U00377
-
-
- HY-146123
-
-
- HY-119938
-
|
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 1 is a potent and non-cytotoxic trypanosoma brucei growth inhibitor with an EC50 of 5 nM.
|
-
- HY-143581
-
-
- HY-13278
-
-
- HY-15775
-
|
|
Arginase
|
Cancer
|
|
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.
|
-
- HY-146387
-
|
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-149989
-
|
|
Ack1
Akt
|
Cancer
|
|
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity.
|
-
- HY-155073
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines).
|
-
- HY-153970
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research.
|
-
- HY-144797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction.
|
-
- HY-146662
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
|
-
- HY-109574
-
|
|
Raf
|
Cancer
|
|
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.
|
-
- HY-133019
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.
|
-
- HY-156969
-
|
|
Btk
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK.
|
-
- HY-132884
-
|
|
Others
|
Cancer
|
|
TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
|
-
- HY-153661
-
-
- HY-111506
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively.
|
-
- HY-13280
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC50 of 160 nM.
|
-
- HY-18928
-
|
|
FAK
|
Cancer
|
|
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
|
-
- HY-121086
-
-
- HY-47026
-
|
|
Others
|
Others
|
|
Protein kinase inhibitor 6 is a protein kinase inhibitor.
|
-
- HY-111489
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-U00370
-
-
- HY-111489A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP inhibitor 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-111489B
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-147761
-
|
|
Flavivirus
Antibiotic
|
Infection
|
|
GAK inhibitor 2 (Compound 14g) is a potent cyclin G-associated kinase (GAK) inhibitor with an IC50 of 0.024 μM. GAK inhibitor 2 shows antiviral activity with an EC50 of 1.049 μM against dengue virus (DENV).
|
-
- HY-144774
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
|
-
- HY-156863
-
|
|
G Protein-coupled Receptor Kinase (GRK)
|
Cardiovascular Disease
|
|
GRK2 Inhibitor 2 (Compound 8h) is a GRK2 inhibitor (IC50: 19 nM). GRK2 Inhibitor 2 also inhibits Aurora-A (IC50: 137 nM). GRK2 Inhibitor 2 promotes β-AR-mediated cAMP accumulation in GRK2-overexpressed HEK293 cells. GRK2 Inhibitor 2 can be used for research of congestive heart failure (HF).
|
-
- HY-156325
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-62 (Compound R3b) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-62 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 2.97 μM and 3.82 μM, respectively.
|
-
- HY-156337
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-63 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 1.99 μM and 1.92 μM, respectively.
|
-
- HY-153401
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis.
|
-
- HY-153750
-
|
|
Wnt
|
Cancer
|
|
Wnt pathway inhibitor 3 is a potent wnt inhibitor with an IC50 value of 45 nM. Wnt pathway inhibitor 3 shows antiproliferative activity.
|
-
- HY-103218
-
|
|
Others
|
Neurological Disease
|
|
Talsupram (hydrochloride) is a selective norepinephrine inhibitor with high affinity for norepinephrine transporter (NET) and can be used in the study of neuropathic pain.
|
-
- HY-157153
-
-
- HY-144743
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 12 (compound 20) is an orally active and potent ATX (autotaxin) inhibitor, with an IC50 of 1.72 nM. ATX inhibitor 12 effectively alleviates lung structural damage with fewer fibrotic lesions at an oral dose of 60 mg/kg in C57Bl/6J mice. ATX inhibitor 12 can be uesd for idiopathic pulmonary fibrosis (IPF) research.
|
-
- HY-143582
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 9 is a potent inhibitor of ATX. ATX inhibitor 9 is a thickened heteroaryl derivatives compound. Autotaxin (ATX), also known as ENPP2, is a secreted enzyme that is highly expressed mainly in cancer cells, bronchial epithelial cells and alveolar macrophages in the lung. ATX inhibitor 9 has the potential for the research of cancer or fibrous degenerative disease (extracted from patent WO2021078227A1, compound 3).
|
-
- HY-144366
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.
|
-
- HY-114317
-
|
|
AMPK
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent and selective microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-130255
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM.
|
-
- HY-153973
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 2 (example 118) is a WRN (Werner Syndrome ATP dependent helicase enzyme) inhibitor, with pIC50 ≥ 7.0.
|
-
- HY-111410
-
-
- HY-153706
-
-
- 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-150983
-
|
|
ATP Synthase
Bacterial
|
Infection
|
|
ATP synthase inhibitor 2 is a Pseudomonas aeruginosa (PA) ATP synthase inhibitor (IC50=10 μg/mL). ATP synthase inhibitor 2 can inhibit Pseudomonas aeruginosa (PA) ATP synthesis activity completely at 128 μg/mL.
|
-
- HY-153593
-
|
|
Epigenetic Reader Domain
|
Cancer
|
BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
|
-
- HY-143461
-
|
|
Casein Kinase
|
Cancer
|
|
CK2 inhibitor 3 is a potent CK2 inhibitor with IC50 value of 280 nM. CK2 inhibitor 3 inhibits endocellular CK2, significantly affects viability of tumour cells and shows remarkable selectivity on a panel of 320 kinases.
|
-
- HY-151421
-
|
|
Fungal
|
Cancer
Infection
|
|
Chitin synthase inhibitor 11 is a chitin synthase inhibitor. Chitin synthase inhibitor 11 shows excellent chitin synthase inhibitory activity with an IC50 value of 0.10 mM. Chitin synthase inhibitor 11 has broad-spectrum antifungal activity in vitro. Chitin synthase inhibitor 11 can be used for the research of invasive fungal infections (IFIs).
|
-
- HY-143265
-
|
|
Topoisomerase
Apoptosis
Caspase
|
Cancer
|
|
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
|
-
- HY-149376
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM，24 h) mediates mitotic arrest，blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa，MCF7，and U87 MG cells.
|
-
- HY-112460
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an 50 of 60 nM.
|
-
- HY-146064
-
|
|
Others
|
Cancer
|
|
OPN expression inhibitor 1 (Compound 11) is an osteopontin (OPN) expression inhibitor. OPN expression inhibitor 1 can be used for breast cancer research.
|
-
- HY-41648
-
-
- HY-128580
-
|
|
FAK
|
Cancer
|
|
FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM, with antitumor and anti-angiogenesis activities.
|
-
- HY-143715
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
|
-
- HY-126134
-
-
- HY-156877
-
-
- HY-153752
-
|
|
Ser/Thr Protease
|
Cancer
|
|
TAO Kinase inhibitor 2 (Example 49) is a TAO Kinase inhibitor (IC50=between 50 and 500 nM). TAO Kinase inhibitor 2 also inhibits KIAA1361 and JIK with IC50s of 50-500 nM.
|
-
- HY-151985
-
|
|
Apoptosis
|
Cancer
|
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity.
|
-
- HY-107662
-
|
|
Apoptosis
|
Cancer
Infection
|
|
TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrP C) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis.
|
-
- HY-146497
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones.
|
-
- HY-151432
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.
|
-
- HY-149498
-
-
- HY-153743
-
|
|
Trk Receptor
ROS Kinase
|
Cancer
|
|
Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively).
|
-
- HY-115970
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 21 (compound 6f), a chalcone- and melatonin- based hybrid, is a potent tubulin inhibitor. Tubulin inhibitor 21 induces a remarkable cytotoxic activity toward SW480 cells (IC50=0.26 μM) with lower effect against nonmalignant cells.
|
-
- HY-112712
-
|
|
HCV
|
Infection
|
|
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a.
|
-
- HY-146671
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC50s of 5.6, 25 nM for ITK, BTK, respectively.
|
-
- HY-146648
-
|
|
HCV
|
Infection
|
|
Cyclophilin inhibitor 3 (compound 7c) is a potent cyclophilin A (CypA) inhibitor with an potent anti-HCV activity (EC50 of 4.2 μM).
|
-
- HY-101053
-
|
Src Kinase Inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-147710
-
|
|
MicroRNA
|
Cancer
|
|
PIN1 inhibitor 2 (compound 12) is a potent PIN1 inhibitor. PIN1 inhibitor 2 shows antitumor activity with an IC50 of 9.55 µM for MCF7 cells. PIN1 inhibitor 2 has the potential for the research of breast cancer.
|
-
- HY-119592
-
-
- HY-157229
-
|
|
EGFR
|
Others
|
|
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants.
|
-
- HY-N0491
-
|
|
nAChR
|
Neurological Disease
|
|
(-)-Sparteine (sulfate) is a quinolizidine alkaloid that can be extracted from Lupinus. (-)-Sparteine (sulfate) inhibits the release of acetylcholine and has anticonvulsant effects.
|
-
- HY-143301
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer.
|
-
- HY-155472
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 17 is a Mcl-1 protein inhibitor. Mcl-1 inhibitor 17 can be used for the research of cancer and other diseases.
|
-
- HY-148058
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells.
|
-
- HY-151418
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 8 is a chitin synthase (CHS) inhibitor with broad-spectrum antifungal activity. Chitin synthase inhibitor 8 can be used in the research of fungi infection.
|
-
- HY-151419
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 9 is a chitin synthase (CHS) inhibitor with broad-spectrum antifungal activity. Chitin synthase inhibitor 9 can be used in the research of fungi infection.
|
-
- HY-146348
-
|
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent.
|
-
- HY-49071
-
|
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 12 (compound 12) is an oxadiazole derivative and an inhibitor of Mycobacterium tuberculosis. The inhibition rates of Tuberculosis inhibitor 12 (20 μM) on 7H9-Tw-OADC and 7H9-Tw-OADC reached 82% and 78% respectively.
|
-
- HY-112270
-
-
- HY-144375
-
|
|
MAGL
|
Others
|
|
Monoacylglycerol lipase inhibitor 1 is a potent monoacylglycerol lipase inhibitor (compound 13).
|
-
- HY-U00319
-
-
- HY-112269
-
-
- HY-153423
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 12 (Example 10) is a MCL-1 inhibitor (Ki: 0.22 nM). Mcl-1 inhibitor 12 can be used for the research of cancers.
|
-
- HY-154988
-
|
|
Others
|
Cancer
Neurological Disease
|
|
MARK4 inhibitor 4 is a MARK4 inhibitor with an IC50 of 1.49 μM. MARK4 inhibitor 4 can be used in cancer and tau lesion-related research.
|
-
- HY-153423A
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 13 (Example 9) is a MCL-1 inhibitor (Ki: 8.2 nM). Mcl-1 inhibitor 13 can be used for the research of cancers.
|
-
- HY-153971
-
|
|
URAT1
|
Metabolic Disease
|
|
URAT1 inhibitor 8 (example 247) is a potent URAT1 inhibitor, with an IC50 of 0.001 μM. URAT1 inhibitor 8 can be used for gout research.
|
-
- HY-150686
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 4 (compound 4fh) is a chitin synthase inhibitor with fungicidal effect. Chitin synthase inhibitor 4 is a potential chitin synthase-based fungicide in agriculture.
|
-
- HY-149981
-
|
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia.
|
-
- HY-150570
-
|
|
Carbonic Anhydrase
CDK
|
Cancer
|
|
Carbonic anhydrase inhibitor 14 (Compound 8b) is a carbonic anhydrase (CA) inhibitor with Ki values of 1203, 99.7, 9.4 and 27.7 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 14 can also inhibit CDK2 with an IC50 of 20.3 μM. Carbonic anhydrase inhibitor 14 shows antitumor activity.
|
-
- HY-146316
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases.
|
-
- HY-160007
-
|
|
Others
|
Cancer
|
|
DHX9-IN-3 (Compound 621) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research.
|
-
- HY-155353
-
|
|
Others
|
Cancer
|
|
ZINC000014708529 is a specific SIRT7 inhibitor with high affinities to SIRT7. ZINC000014708529 can be used in the research against cancers.
|
-
- HY-160008
-
|
|
Others
|
Cancer
|
|
DHX9-IN-4 (Compound 609) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research.
|
-
- HY-156795
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK9/CycT1 Degrader-2 is a inhibitor of CDK9, with the IC50 of 45 nM.
|
-
- HY-149486
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor 7 (compound 5) is an inhibitor of FGFR1 Tyrosine Kinase with IC50 value of 0.33 nM. FGFR1 inhibitor 7 shows broad-spectrum cytotoxicity agasinst human cancer cell lines, and inhibits MOLT3 cells with IC50 of 2.1 μM.
|
-
- HY-155645
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 15 (compound 2g) is a Topoisomerase II inhibitor. Topoisomerase II inhibitor 15 potently is an apoptotic inducer with greater selectivity against head and neck tumors.
|
-
- HY-147649
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 7 (Compound 6) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 3.65 μM. Glyoxalase I inhibitor 7 can be used as anticancer agent.
|
-
- HY-144376
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 4 is carbonic anhydrase photoprobe/inhibitor. Carbonic anhydrase inhibitor 4 is against human carbonic anhydrases (hCA I-XIV) with Ki values of 640-1166 nM.
|
-
- HY-147877
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity.
|
-
- HY-U00439
-
|
|
DYRK
|
Cancer
|
|
Protein kinase inhibitor 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
|
-
- HY-101791
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
|
-
- HY-153745A
-
|
|
Trk Receptor
|
Cancer
|
|
Protein kinase inhibitor 5 sulfate hydrate is a potent TRK-A inhibitor with an IC50 value of 1.8 nM. Protein kinase inhibitor 5 sulfate hydrate inhibits cell viability.
|
-
- HY-148836
-
|
|
c-Myc
|
Cancer
Infection
Cardiovascular Disease
|
|
c-Myc inhibitor 6 (compound A102) is a c-Myc inhibitor. c-Myc inhibitor 6 decreases cancer cell viability and degrades c-Myc protein. c-Myc inhibitor 6 can be used for the research of c-Myc imbalance, such as cancer, cardiovascular diseases, and viral infection.
|
-
- HY-153348
-
|
|
p38 MAPK
|
Cancer
|
|
p38 Kinase inhibitor 4 (compound 135) is a potent p38 inhibitor.
|
-
- HY-128311
-
-
- HY-P6013
-
|
|
Calcium Channel
|
Others
|
|
wt hMLN is a microprotein that inhibits of SR Ca 2+ pump (SERCA). wt hMLN plays an important role in skeletal muscle calcium homeostasis.
|
-
- HY-156784
-
|
|
Others
|
Cancer
|
|
DHX9-IN-2 is an inhibitor of ATP-dependent RNA helicase A (DHX9), with the IC50 of 0.0698 nM that has antitumor activity.
|
-
- HY-156782
-
|
|
Others
|
Cancer
|
|
DHX9-IN-1 is an inhibitor of ATP-dependent RNA helicase A (DHX9), with the IC50 of 9.45 nM that has antitumor activity.
|
-
- HY-149673
-
|
|
CDK
|
Cancer
|
|
XPW1 is a potent and selective CDK9 inhibitor with excellent activity against clear cell renal cell carcinoma (ccRCC) and low toxicity.
|
-
- HY-156464
-
|
|
Topoisomerase
|
Infection
|
|
Topoisomerase I inhibitor 10 (compound 13) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 10 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 27.91 μM.
|
-
- HY-154962
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 15 (Compound (Ra)-15) is a Mcl-1 inhibitor (Ki: 0.02 nM). Mcl-1 inhibitor 15 can be used for research of cancer.
|
-
- HY-114309
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.
|
-
- HY-147647
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 5 (Compound 9h) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.28 μM. Glyoxalase I inhibitor 5 can be used as anticancer agent.
|
-
- HY-128726
-
|
|
Itk
|
Inflammation/Immunology
|
|
ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM.
|
-
- HY-14177
-
|
|
Raf
|
Cancer
|
|
Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
|
-
- HY-156359
-
|
|
Others
|
Others
|
|
Tuberculosis inhibitor 10 shows moderate inhibitory effect on the enzymatic activity of MSMEG_6649. Tuberculosis inhibitor 10 enhances the inhibitory activity of PAS against mycobacteria.
|
-
- HY-144452
-
|
|
Proteasome
|
Cancer
|
|
Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases.
|
-
- HY-151416
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 6 (compound 9b) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.21 mM. Chitin synthase inhibitor 6 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 6 can be used in the research of fungi infection.
|
-
- HY-155507
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 11 (Compound 67e) is a c-MYC inhibitor (pEC50: 6.4). c-Myc inhibitor 11 has high clearance levels, moderate volume of distribution and short half-life in rat pharmacokinetic assay. c-Myc inhibitor 11 can be used for cancer research.
|
-
- HY-115994
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research.
|
-
- HY-149813
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 14 (Compound 8a) is a high affinity P-gp inhibitor. P-gp inhibitor 14 reverses P-gp-mediated multidrug resistance (EC50=48.74 nM). P-gp inhibitor 14 has a weak inhibitory effect on CYP3A4 activity.
|
-
- HY-151417
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 7 (compound 9c) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.37 mM. Chitin synthase inhibitor 7 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 7 can be used in the research of fungi infection.
|
-
- HY-146386
-
|
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-146437
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases.
|
-
- HY-151420
-
|
|
Fungal
|
Cancer
Infection
|
|
Chitin synthase inhibitor 10 is a chitin synthase inhibitor. Chitin synthase inhibitor 10 shows excellent chitin synthase inhibitory activity with an IC50 value of 0.11 mM. Chitin synthase inhibitor 10 also is an antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 10 can be used for the research of invasive fungal infections (IFIs).
|
-
- HY-151422
-
|
|
Fungal
|
Cancer
Infection
|
|
Chitin synthase inhibitor 12 is a chitin synthase inhibitor. Chitin synthase inhibitor 12 shows excellent inhibitory activity with an IC50 value of 0.16 mM. Chitin synthase inhibitor 12 also is a broad-spectrum antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 12 can be used for the research of invasive fungal infections (IFIs).
|
-
- HY-50670
-
-
- HY-146037
-
|
|
Apoptosis
Aurora Kinase
|
Cancer
|
|
Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells.
|
-
- HY-146654
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 2 (compound 26) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.5 µM. Glyoxalase I inhibitor 2 has the potential for the research of depression and anxiety.
|
-
- HY-155569
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 13 (compound 12g) is a non-competitive inhibitor of chitin synthase, with an IC50 of 106.7 μM. Chitin synthase inhibitor 13 exhibits a broad-spectrum of antifungal activity.
|
-
- HY-149635
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC50 values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA.
|
-
- HY-14177A
-
|
|
Raf
|
Cancer
|
|
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
|
-
- HY-144189
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5， such as cancer.
|
-
- HY-157227
-
|
VPC4
|
Others
|
Others
|
|
VPC01091.4 is a TRPM7 inhibitor. VPC01091.4 is an efficacious anti-inflammatory agent that arrests systemic inflammation in vivo.
|
-
- HY-156040
-
|
|
Casein Kinase
|
Cancer
|
|
Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685).
|
-
- HY-155231
-
|
|
Elastase
|
Cancer
|
|
Neutrophil elastase inhibitor 4 (compound 4f) is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM). Neutrophil elastase inhibitor 4 induces T47D cell apoptosis. Neutrophil elastase inhibitor 4 inhibits cell proliferation with IC50s of 21.25, 34.17, 29.93, 99.11 nM for T47D, RPMI 8226, A549, and HSF cells.
|
-
- HY-151410
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 5 (compound 9a) is an inhibitor of chitin synthase with an IC50 value of 0.14 mM. Chitin synthase inhibitor 5 shows broad-spectrum antifungal activity in vitro and shows good inhibition to C. albicans, A. flavus, A. fumigatus and C. neoformans. Chitin synthase inhibitor 5 can be used for the research of fungal.
|
-
- HY-132175
-
|
|
Casein Kinase
|
Cancer
|
|
CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
|
-
- HY-149585
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 14 (compound 4n) is chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 14 has antifungal activity while possessed the potency against drug-resistant fungal variants.
|
-
- HY-149425
-
|
|
Sirtuin
|
Cancer
Inflammation/Immunology
|
|
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC50 of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo.
|
-
- HY-147812
-
|
|
Others
|
Cancer
|
|
POLA1 inhibitor 1 (Compound 12) is an orally active POLA1 inhibitor. POLA1 inhibitor 1 shows antitumor activity against several tumor histotypes and Adarotene-resistant cell line.
|
-
- HY-147648
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 6 (Compound 9j) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.13 μM. Glyoxalase I inhibitor 6 can be used as anticancer agent with low toxicity.
|
-
- HY-156462
-
|
|
Topoisomerase
|
Infection
|
|
Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM.
|
-
- HY-146655
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 3 (compound 22g) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.011 µM. Glyoxalase I inhibitor 3 has the potential for the research of depression and anxiety.
|
-
- HY-146163
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis.
|
-
- HY-112634
-
|
|
Sirtuin
|
Others
|
|
SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM.
|
-
- HY-146656
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 4 (compound 14) is a potent glyoxalase I inhibitor with an Ki of 10 nM.
|
-
- HY-144988
-
|
|
CD38
|
Cancer
|
|
CD38 inhibitor 2 is a potent CD38 inhibitor (IC50 = 0.01 ~ 0.1 μΜ).
|
-
- HY-111493
-
-
- HY-123538
-
-
- HY-115998
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 11 (compound VI) is a potent, selective carbonic anhydrase inhibitor. Carbonic anhydrase inhibitor 11 shows Ki values of 40, 39, 200 and 900 nM against CA II, IX, and XII, respectively.
|
-
- HY-112715
-
|
|
ATP Synthase
|
Cardiovascular Disease
|
|
ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels.
|
-
- HY-129167
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction extracted from patent WO2017214367, compound example 1. Menin-MLL inhibitor 4 has antitumor activity.
|
-
- HY-157123
-
|
|
Tyrosinase
|
Others
|
Tyrosinase-IN-18 (compound 6) is a potent tyrosinase inhibitor. Tyrosinase-IN-18 has strong antioxidant activities against ROS, ABTS+, and DPPH radicals.
|
-
- HY-90009D
-
|
cis-ent-IC-351; Tadalafil, (6S,12aR)-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
cis-ent-Tadalafil (Tadalafil EP Impurity C) is a highly potent PDE5 inhibitor with an IC50 value of 5 nM and has blood pressure lowering activity.
|
-
- HY-149720
-
-
- HY-143306
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively.
|
-
- HY-155202
-
|
|
Others
|
Others
|
|
YJ196 (Compound 59) is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor.
|
-
- HY-22166
-
|
|
Others
|
Metabolic Disease
|
|
Glycolic acid oxidase inhibitor 1 is a glycolate oxidase inhibitor, extracted from patent EP0021228A1, in Table IV.
|
-
- HY-143281
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer activities.
|
-
- HY-155508
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 12 (compound 67h) is an inhibitor of c-Myc with a pEC50 of 6.4.
|
-
- HY-13275
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
|
-
- HY-148203
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 9 (example 2) is a myeloid cell leukemia 1 (Mcl-1) inhibitor with IC50 value of 0.21889 nM. Mcl-1 inhibitor 9 shows anti-tumor activity.
|
-
- HY-144391
-
|
|
Fungal
Antibiotic
|
Inflammation/Immunology
|
|
Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor (IC50=0.12 mM). Chitin synthase inhibitor 1 has potent antifungal activity against drug-resistant fungi variants.
|
-
- HY-143246
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.
|
-
- HY-149976
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 4 (Compound 10f) is a Pim-1 kinase inhibitor (IC50: 17.01 nM). Pim-1 kinase inhibitor 4 also has antioxidant activity and inhibits DPPH. Pim-1 kinase inhibitor 4 induces apoptosis in PC-3 cell, and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used for research of prostate cancer.
|
-
- HY-101998
-
|
|
Others
|
Metabolic Disease
|
|
CTP inhibitor is a potent and selective CTP inhibitor. CTP inhibitor inhibits the plasma membrane citrate transporter (PMCT).
|
-
- HY-135899
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
|
-
- HY-153969
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 6 (Compound 1h) is a potent URAT1 inhibitor (IC50: 35 nM for hURAT1). URAT1 inhibitor 6 is 200- and 8-fold more potent than parent Lesinurad (HY-15258) and Benzbromarone (HY-B1135). URAT1 inhibitor 6 can be used for research of inflammation.
|
-
- HY-148909
-
|
IDEFP
|
FAAH
Cannabinoid Receptor
|
Neurological Disease
|
|
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM).
|
-
- HY-121933
-
|
|
Aldose Reductase
|
Metabolic Disease
|
|
IDD388 is a selective aldose reductase (ALR2) inhibitor with an IC50 of 30 nM. IDD388 displays selectivity for ALR2 over ALR1 (IC50 of 14 μM).
|
-
- HY-18297
-
-
- HY-155235
-
|
|
Others
|
Cancer
|
|
Steroid sulfatase-IN-7 is an irreversible steroid sulfatase (STS) inhibitor with an IC50 value of 0.05 nM against human placental STS and can be used in cancer research.
|
-
- HY-157226
-
|
|
Others
|
Others
|
|
ORI-TRN-002 is an AQP4 inhibitor with an IC50 value of 3μM. ORI-TRN-002 can be used in the research area of cerebral edema.
|
-
- HY-149623
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bcl-2-IN-13 is a Bcl-2 inhibitor with an IC50 value of 17 nM. Bcl-2-IN-13 can be used in cancer research.
|
-
- HY-151524
-
|
|
Cathepsin
|
Inflammation/Immunology
|
|
Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies.
|
-
- HY-10644
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively
|
-
- HY-114418
-
|
|
MMP
|
Cancer
|
|
MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM.
|
-
- HY-150238
-
-
- HY-151372
-
|
|
PKD
|
Cancer
|
|
Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation.
|
-
- HY-152033
-
|
|
URAT1
GLUT
|
Metabolic Disease
|
|
URAT1 inhibitor 4, a Lesinurad derivative, is a potent and orally active URAT1 inhibitor with an IC50 of 7.56 μM. URAT1 inhibitor 4 has higher in vivo urate-lowering efficacy than Lesinurad (HY-15258).
|
-
- HY-155012
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 16 (Compound 9) is a mitochondrial targeting Platinum-based inhibitor of Mcl-1. Mcl-1 inhibitor 1 induces Bax/Bak-dependent apoptosis in cancer cells. Mcl-1 inhibitor 16 can be used alone or together with ABT-199 (HY-15531) and shows anti-tumor activity.
|
-
- HY-146189
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells.
|
-
- HY-149642
-
|
|
Dihydroorotate Dehydrogenase
|
Others
|
|
hDHODH-IN-13 (compound w2) is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 value of 173.4 nM. hDHODH-IN-13 can be used in the research of IBD.
|
-
- HY-157128
-
|
|
PI3K
|
Inflammation/Immunology
|
Se15 is a selective inhibitor of PI3Kδ with an IC50 value less than 0.1nM. Se15 can be used in research on autoimmune.
|
-
- HY-122167
-
-
- HY-137495
-
|
|
PAI-1
Ser/Thr Protease
|
Cancer
|
|
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.
|
-
- HY-128798
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, Intermediate 6).
|
-
- HY-112297
-
-
- HY-149293
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Skp2 inhibitor 1 (compound 14i) is a potent and selective Skp2 inhibitor against the Skp2-Cks1 interaction with an IC50 of 2.8 μM. Skp inhibitor 1 exhibits anticancer activity.
|
-
- HY-149002
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
|
-
- HY-156243
-
|
|
Others
|
Cancer
|
|
GDI2-IN-1 (compound (+)-37) is a GDP-dissociation inhibitor beta (GDI2) inhibitor with an IC50 of 2.87 μM and a KD of 36 μM. GDI2-IN-1 exhibits excellent in vivo antitumor activity in GDI2-overexpressing pancreatic xenograft models.
|
-
- HY-146504
-
|
|
Topoisomerase
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.
|
-
- HY-150775
-
|
|
Cytochrome P450
|
Cancer
|
|
Nonsteroidal aromatase inhibitor 1 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). Nonsteroidal aromatase inhibitor 1 has potential for breast cancer research. Nonsteroidal aromatase inhibitor 1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-156120
-
|
|
CD38
|
Metabolic Disease
|
|
CD38 inhibitor 3 (compound 1) is a potent CD38 inhibitor (IC50=11 nM). CD38 inhibitor 3 can promote mitochondrial biogenesis, reduce lactate levels, and increase NAD+ content and Nrf2 expression. In a model of mitochondrial myopathy, CD38 inhibitor 3 increases muscle contraction/development and improves exercise tolerance in Pus1 -/- mice.
|
-
- HY-149491
-
|
|
HIF/HIF Prolyl-Hydroxylase
TAM Receptor
|
Others
|
|
Axl-IN-16 (Compound 4) is a Axl inhibitor. Axl-IN-16 inhibits Axl expression and inhibits the activity of HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 can be isolated from“fruiting liquid (FL)” of Hypholoma lateritium and Hericium erinaceus.
|
-
- HY-103032
-
|
|
PDGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
|
-
- HY-15735
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
|
-
- HY-149509
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 9 (Compound 20C) is an α-Synuclein inhibitor. α-Synuclein inhibitor 9 binds to cavities in mature α-synuclein fibrils and reduces the β-sheet structure. α-Synuclein inhibitor 9 inhibits A53T α-Syn aggregation. α-Synuclein inhibitor 9 has neuroprotective effect, improves brain functional connection and relieves motor dysfunction.α-Synuclein inhibitor 9 can be used for Parkinson’s disease (PD) research..
|
-
- HY-150583
-
|
|
Fungal
Antibiotic
|
Inflammation/Immunology
|
|
Chitin synthase inhibitor 2 (compound 2b) is a potent inhibitor of chitin synthase with the IC50 value of 0.09 mM and the Ki value of 0.12 mM. Chitin synthase inhibitor 2 has antimicrobial activities in vitro and shows synergistic or additive effects with fluconazole or polyoxin B.
|
-
- HY-155693
-
|
|
Topoisomerase
Parasite
|
Infection
|
|
Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research.
|
-
- HY-N144114
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC50=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300).
|
-
- HY-147031
-
|
|
Deubiquitinase
|
Cancer
|
|
JAMM protein inhibitor 2 (compound 180) is a potent JAMM protease inhibitor with IC50s of 10 μM, 46 μM and 89 μM for thrombin, Rpn11 and MMP2, respectively. JAMM protein inhibitor 2 can be used for researching anticancer
|
-
- HY-146188
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase.
|
-
- HY-112701
-
|
|
CCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
|
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.
|
-
- HY-163015
-
|
|
Others
|
Infection
|
|
RNA polymerase-IN-1 (compound 4) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-1 inhibits CYP isozymes.
|
-
- HY-163016
-
|
|
Others
|
Infection
|
|
RNA polymerase-IN-2 (compound 5) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-2 inhibits CYP isozymes.
|
-
- HY-153577
-
-
- HY-152031
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Glutaminyl Cyclase Inhibitor 5 (Compound 71) is a potent and selective human glutaminyl cyclase (hQC) inhibitor with an IC50 of 3.2 nM.
|
-
- HY-112432
-
|
|
GlyT
|
Neurological Disease
|
|
GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC50 of 38 nM for rGlyT1. Antipsychotic activity.
|
-
- HY-103079
-
|
|
Phosphatase
|
Cancer
|
|
PRL-3 Inhibitor 2 (compound 2) is a potent PRL-3 inhibitor with an IC50 value of 28.1 µM.
|
-
- HY-126142
-
-
- HY-150044
-
|
|
DNA/RNA Synthesis
Topoisomerase
Bacterial
|
Infection
|
|
Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
|
-
- HY-157152
-
|
|
HDAC
|
Cancer
|
HDAC-IN-65 ( compound 6) is a selective histone deacetylase (HDAC) inhibitor with IC50 value of 2.5μM. HDAC-IN-65 is a prodrug with very good bioreductive properties.
|
-
- HY-145231
-
|
|
FGFR
|
Cancer
|
|
FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor with IC50s of 389, 29, and 758 nM for FGFR1, FGFR2, and FGFR3, respectively.
|
-
- HY-100231
-
|
|
Cathepsin
|
Cancer
|
|
Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively.
|
-
- HY-112569
-
-
- HY-147785
-
|
|
Pim
Apoptosis
|
Cancer
|
|
Pim-1 kinase inhibitor 2 (Compound 13) is a potent inhibitor of Pim-1 kinase. Pim-1 kinase inhibitor 2 induces apoptosis. Pim-1 kinase inhibitor 2 has the potential for the research of cancer diseases.
|
-
- HY-147908
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR.
|
-
- HY-147907
-
|
|
Adenosine Receptor
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.
|
-
- HY-150565
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
|
-
- 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-148837
-
|
|
c-Myc
Casein Kinase
|
Cancer
Infection
Cardiovascular Disease
|
|
c-Myc inhibitor 7 is a c-Myc inhibitor and a multiple target protein degrader. c-Myc inhibitor 7 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. c-Myc inhibitor 7 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection.
|
-
- HY-139076
-
|
|
Epigenetic Reader Domain
|
Cancer
Metabolic Disease
|
|
Menin-MLL inhibitor 19, a potent exo-aza spiro inhibitor of menin-mll interaction, example A17, extracted from patent WO2019120209A1. Menin-MLL inhibitor 19 can be used for the reseaech of various diseases, such as cancer, myelodysplastic syndrome (MDS) and diabetes.
|
-
- HY-155414
-
|
|
Elastase
|
Inflammation/Immunology
|
|
Neutrophil elastase inhibitor 5 (compound 29) is a dual inhibitor of HNE (human neutrophil elastase) and proteinase 3 (PR3) with IC50 values of 4.91 μM and 20.69 μM, respectively. Neutrophil elastase inhibitor 5 can be used in the study of neutrophil inflammatory diseases.
|
-
- HY-143266
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.
|
-
- HY-112722
-
-
- HY-145825
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 7 is a potent Mcl-1 inhibitor, example 35, extracted from patent WO2020097577A.
|
-
- HY-126146
-
|
|
PKC
|
Cancer
|
|
PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ℩) inhibitor with an IC50 value of 0.34 μM.
|
-
- HY-132181
-
|
|
Na+/H+ Exchanger (NHE)
|
Inflammation/Immunology
|
|
Dimethylamiloride hydrochloride is a Na +/H + exchanger NHE inhibitor with Ki values of 0.02, 0.25, and 14 μM for NHE1, NHE2, and NHE3, respectively. Dimethylamiloride hydrochloride can be used for pain research.
|
-
- HY-150983A
-
|
|
ATP Synthase
Bacterial
|
Infection
|
|
ATP synthase inhibitor 2 (Compound 22) TFA is a Pseudomonas aeruginosa (PA) ATP synthase inhibitor (IC50=10 μg/mL). ATP synthase inhibitor 2 TFA can inhibit Pseudomonas aeruginosa (PA) ATP synthesis activity completely at 128 μg/mL.
|
-
- HY-111623
-
|
|
Deubiquitinase
|
Cancer
|
|
USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.
|
-
- HY-W278582
-
|
|
Apoptosis
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 14 (compound 2f) is a potent inhibtor of Topoisomerase II, with anticancer activity. Topoisomerase II inhibitor 14 induces apoptosis, and arrests cell cycle at S phase. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO.
|
-
- HY-156378
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively.
|
-
- HY-13335
-
|
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
|
-
- HY-U00387
-
-
- HY-149542
-
|
|
GSK-3
Apoptosis
Tau Protein
|
Neurological Disease
|
|
GSK-3β inhibitor 15 (Compound 54) is a GSK-3β inhibitor (IC50: 3.4 nM). GSK-3β inhibitor 15 inhibits Aβ1-42-induced GSK-3β and tau protein phosphorylation. GSK-3β inhibitor 15 inhibits LPS-induced iNOS expression. GSK-3β inhibitor 15 has neuroprotective effects on Aβ1-42-induced neurotoxicity. GSK-3β inhibitor 15 can be used for research of Alzheimer’s disease (AD).
|
-
- HY-147861
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity.
|
-
- HY-147839
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells.
|
-
- HY-114414
-
|
|
HDAC
mTOR
Apoptosis
|
Cancer
|
|
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies.
|
-
- HY-155460
-
|
|
Bacterial
|
Infection
|
|
Pks13-TE inhibitor 4 (compound 44) is an oxadiazole series Pks13 inhibitor that effectively inhibits tuberculosis (TB) and resolves its drug resistance.
|
-
- HY-148676
-
|
Menin-MLL Inhibitor 26
|
Epigenetic Reader Domain
|
Cancer
|
|
Emilumenib (Menin-MLL inhibitor 26) is a Menin-MLL inhibitor. Emilumenib also is an active reference. Emilumenib can inhibits cell growth. Emilumenib can be used for the research of leukemia.
|
-
- HY-139536
-
-
- HY-146227
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase.
|
-
- HY-138989
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
15-LOX-1 inhibitor 1 is a potent inhibitor of 15-LOX-1 (15-lipoxygenase-1) with an IC50 value of 0.19 μM. 15-LOX-1 inhibitor 1 protects macrophages from lipopolysaccharide-induced cytotoxicity. 15-LOX-1 inhibitor 1 inhibits NO formation and lipid peroxidation.
|
-
- HY-142452
-
|
|
Raf
|
Cancer
|
|
Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B).
|
-
- HY-154839
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 10 (compound 17), a c-Myc inhibitor, exhibits increased cellular potency, consistent with an increase in permeability with methylation of the morpholine nitrogen.
|
-
- HY-U00439A
-
|
|
DYRK
|
Cancer
|
|
Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-122700
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
|
-
- HY-147940
-
|
|
Parasite
|
Infection
|
|
TbPTR1 inhibitor 1 (compound 5d) is a potent kinetoplastid pteridine reductase 1 (PTR1) inhibitor with an IC50<0.1 nM for TbPTR1. TbPTR1 inhibitor 1 has inhibitory activity against Trypanosoma brucei (EC50=0.66 μM).
|
-
- HY-146653
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 1 (compound 23) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 26 nM. Glyoxalase I inhibitor 1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W009689
-
|
|
Parasite
|
Infection
|
|
TbPTR1 inhibitor 2 (Compound 3a) is a PTR1 enzyme inhibitor, with IC50s of 34.2 and 32.9 μM for TbPTR1 and LmPTR1. TbPTR1 inhibitor 2 has anti-parasitic activity against T. brucei (IC50: 34.2 μM).
|
-
- HY-157132
-
|
|
FAAH
|
Neurological Disease
|
FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity.
|
-
- HY-149624
-
|
|
Others
|
Cancer
|
|
Bcl-2-IN-14 (Compound 13c) is a BCL-2 inhibitor with an IC50 value of 0.471 μM. Bcl-2-IN-14 can be used in cancer research.
|
-
- HY-160006
-
|
|
Pim
|
Cancer
|
|
PIM-IN-2 (Pim-2) is a Pim kinases inhibitor (IC50 = 25 nM). PIM-IN-2 promotes cell survival, is antiapoptotic, and has exhibited an elevated level of expression in a variety of human tumors.
|
-
- HY-157231
-
|
|
PERK
|
Cancer
|
|
HC-5404 is a potent and selective PERK inhibitor. HC-5404 has orally activity. HC-5404 significantly blocks metastasis via killing quiescent/slow-cycling ISRhigh.
|
-
- HY-132920
-
|
|
Ras
|
Cancer
|
|
KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential research in cancer.
|
-
- HY-148133
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 12 (compound 15) is an inhibitor of GSK-3β. GSK-3β inhibitor 12 inhibits 49.11% and 37.11% activity of 25 μM and 50 μM GSK-3β, respectively. GSK-3β inhibitor 12 can be used for the research of neurodegenerative diseases.
|
-
- HY-150079
-
|
|
HIV Integrase
|
Infection
|
|
HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).
|
-
- HY-11059
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity.
|
-
- HY-143713
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora A inhibitor 1 is a potent and selective inhibitor of Aurora A. Aurora A has been implicated in cancers of diverse histological origin and may possess oncogenic properties when overexpressed. Aurora A inhibitor 1 has the potential for the research of cancer diseases mediated by aurora a (extracted from patent WO2021147974A1, compound 49).
|
-
- HY-131068
-
-
- HY-144807
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity.
|
-
- HY-149850
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
p38 Kinase inhibitor 5 (AA6) is a potent p38 kinase inhibitor with an IC50 of 403.57 nM. p38 Kinase inhibitor 5 has anti-inflammatory activity.
|
-
- HY-153435
-
|
|
RIP kinase
Necroptosis
|
Cancer
|
|
RIP1 kinase inhibitor 5 (example 1) is a potent inhibitor of RIP1, which is used as a checkpoint kinase to control tumor immunity. RIP1 kinase inhibitor 5 is similar with SIR1-365 (compound 13), which inhibits necrosis and iron death activity.
|
-
- HY-155804
-
|
|
RIP kinase
Necroptosis
|
Inflammation/Immunology
|
|
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species.
|
-
- HY-114147
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against agent-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability.
|
-
- HY-132307
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
|
-
- HY-P10061
-
|
|
Cathepsin
|
Cancer
|
|
Cathepsin K inhibitor 4 is a potent carbohydrazide Cathepsin K inhibitor with IC50s of 13 nM, 269 nM, 296 nM for human, rat, mouse Cathepsin K, respectively.
|
-
- HY-128661
-
-
- HY-153688
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
SORT-PGRN interaction inhibitor 3 (Compound 13) is a SORT-PGRN interaction inhibitor (IC50: 0.17 μM). SORT-PGRN interaction inhibitor 3 can be used for research of neurodegenerative diseases.
|
-
- HY-145825A
-
|
|
Bcl-2 Family
|
Cancer
|
|
(E)-Mcl-1 inhibitor 7 (Example 34) is a Mcl-1 inhibitor (Ki: <1 nM, IC50: <500 nM). (E)-Mcl-1 inhibitor 7 can be used for research of cancers.
|
-
- HY-147633
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 52 (Compound 7) is a KRAS G12C inhibitor.
|
-
- HY-147636
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 55 (Compound 1) is a KRAS G12C inhibitor.
|
-
- HY-147632
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 51 (example 1) is a KRAS G12C inhibitor.
|
-
- HY-147635
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor.
|
-
- HY-147634
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 53 (Compound 1) is a KRAS G12C inhibitor.
|
-
- HY-123669
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
R-138727, the thiol-containing active metabolite of Prasugrel, is an irreversible platelet P2Y12 receptor inhibitor. R-138727 inhibits ADP-induced platelet aggregation.
|
-
- HY-12202
-
|
|
MEK
|
Cancer
|
|
MEK inhibitor is a potent MEK inhibitor with antitumor potency.
|
-
- HY-147644
-
|
|
Others
|
Neurological Disease
|
|
α-Synuclein inhibitor 3 (Compound 7g) is a α-synuclein (α -Syn) aggregation inhibitor. α-Synuclein inhibitor 3 can be used for Parkinson’s disease research.
|
-
- HY-146204
-
|
|
HIV
|
Infection
|
|
HIV-1 capsid inhibitor 1 is a potent HIV-1 Capsid inhibitor with an EC50 value of 3.13 µM. HIV-1 capsid inhibitor 1 shows antiviral activities.
|
-
- HY-U00304
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor extracted from patent WO2007059299A1, compound 1-3, has a Ki value of <0.010 uM.
|
-
- HY-107485
-
-
- HY-142947
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 45 (compound 78) is a potent KRAS G12C inhibitor.
|
-
- HY-130254
-
|
|
Src
|
Cancer
Inflammation/Immunology
|
|
Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
|
-
- HY-143793
-
|
|
Others
|
Metabolic Disease
|
|
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice.
|
-
- HY-143714
-
|
|
Cathepsin
|
Inflammation/Immunology
|
|
Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).
|
-
- HY-129189
-
|
|
Ras
|
Cancer
|
|
RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
|
-
- HY-133015
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity..
|
-
- HY-100556
-
|
|
Tie
|
Cancer
|
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-136010
-
|
|
RIP kinase
PROTACs
|
Inflammation/Immunology
|
|
RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α.
|
-
- HY-131061
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity.
|
-
- HY-119996
-
|
|
Others
|
Inflammation/Immunology
|
|
AR-C141990 (Compound 30) is a potent blocker of the monocarboxylate transporter MCT1 with a Ki of 4.8 nM. AR-C141990 (Compound 30) inhibits CYP3A4 and CYP2C9 with IC50 values of 16 μM.
|
-
- HY-103673
-
|
|
Adenosine Deaminase
|
Neurological Disease
|
|
AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in the research of sugar craving, salt craving, umami craving, and addictions including agent, tobacco, nicotine and alcohol addictions.
|
-
- HY-150584
-
|
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 3 (compound 2d) is a potent chitin synthase inhibitor with an IC50 value of 0.16 mM, and MIC of 1 µg/mL against candida albicans. Antifungal activity.
|
-
- HY-107977
-
-
- HY-150727
-
|
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively.
|
-
- HY-123999
-
|
|
CD38
|
Metabolic Disease
|
|
CD38 inhibitor 1 (compound 78c) is a potent CD38 inhibitor with IC50s of 7.3 nM and 1.9 nM for hCD38 and mouse CD38.
|
-
- HY-111507
-
|
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-142948
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 46 (compound WX003) is a potent KRAS G12C inhibitor.
|
-
- HY-115213
-
-
- HY-157150
-
|
|
Adenylate Cyclase
|
Infection
|
|
mAC2-IN-1 (compound 14) is a potent and selective human adenylate cyclases (mACs) inhibitor with an IC50 of 4.45 μM. mAC2-IN-1 has low activity on mAC1 and mAC5.
|
-
- HY-132572
-
|
|
HIV
|
Infection
|
|
HIV-1 integrase inhibitor 9 (compound 8a) is a potent HIV-1 RNase H inhibitor with an IC50 of 12.3 μM. HIV-1 integrase inhibitor 9 shows an antiviral activity.
|
-
- HY-151450
-
-
- HY-152552
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC50 value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity.
|
-
- HY-P4133
-
|
|
ERK
MEK
|
Cancer
|
|
MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable.
|
-
- HY-W096600
-
|
1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos
|
Others
|
Cancer
|
|
2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) acts as a potent fucosyltransferase (FUT) inhibitor.
|
-
- HY-143657
-
|
|
Others
|
Cancer
|
|
Myoferlin inhibitor 1 is a novel agent against pancreatic cancer metastasis through targeting myoferlin.
|
-
- HY-152199
-
|
|
Adenosine Deaminase
|
Metabolic Disease
|
|
AMPD2 inhibitor 2 (compound 21) is a potent AMP deaminase 2 (AMPD2) inhibitor with IC50s of 0.1 μM and 0.28μM for hAMPD2 and mAMPD2, respectively. AMPD2 inhibitor 2 has the potential for evaluating the physiological role of AMPD2 in mice maintained on a high fat diet.
|
-
- HY-154961
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 14 (Compound (Ra)-10) is an inhibitor of myeloid cell leukemia-1 (MCL-1) with an Ki of 0.018 nM and can be used for anticancer research.
|
-
- HY-145020
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1).
|
-
- HY-130795
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-143295
-
|
|
Pim
Apoptosis
|
Cancer
|
|
Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC50 of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer.
|
-
- HY-17542
-
|
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-139139
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A inhibitor 3 is a methionine adenosyltransferase 2A (MAT2A) inhibitor extracted from patent WO2020123395A1, compound 24, has an IC50 of <200 nM. MAT2A inhibitor 3 can be used for the research of cancers.
|
-
- HY-114423
-
-
- HY-N12347
-
|
|
Others
|
Inflammation/Immunology
|
|
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitory activity against α-Glucosidase.
|
-
- HY-11000A
-
|
|
ROCK
|
Cancer
|
|
CaMKP inhibitor sodium is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
|
-
- HY-112441
-
-
- HY-143245
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
|
-
- HY-143244
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study.
|
-
- HY-132980
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1).
|
-
- HY-156361
-
|
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 11 (Compound 14) can sensitize the antimycobacterial activity of the antitubercular agent.
|
-
- HY-155786
-
|
|
TGF-beta/Smad
|
Others
|
|
3,7-DMF is an orally active inhibitor of TGF-β1-induced activation of HSCs. 3,7-DMF induces antioxidant genes and quenches ROS away, which can be used to study liver fibrosis.
|
-
- HY-149722
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-20 (Compound 1p) is a parasite inhibitor with broad antiparasitic activity. Antiparasitic agent-20 has inhibitory effects on T. brucei and T. cruzi with EC50 values of 0.09 μM and 14.1 μM respectively.
|
-
- HY-149719
-
|
|
Ferroptosis
|
Metabolic Disease
|
Ferroptosis-IN-4 (compound 6k) is a ferroptosis inhibitor with EC50 value of 20 μM. Ferroptosis-IN-4 has no obvious cytotoxicity. Ferroptosis-IN-4 has a protective effect in glycerol-induced RM-AKI mice with alleviating kidney dysfunction.
|
-
- HY-120157
-
|
|
HIV
|
Infection
|
|
Vif-ElonginC interaction inhibitor 1 (compound VEC-5) is a potent Vif inhibitor. Vif-ElonginC interaction inhibitor 1 can restrict HIV-1 in Vif-nonpermissive cells. Vif-ElonginC interaction inhibitor 1 can protect A3G, APOBEC3C (A3C), and APOBEC3F (A3F) from Vif-mediated degradation and drastically inhibit Vif function through blocking the interaction between Vif and ElonginC. Vif-ElonginC interaction inhibitor 1 enhances A3G incorporation into HIV-1 virions to reduce viral infectivity.
|
-
- 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-129682
-
-
- HY-149641
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-29 (compound Z11) is a potent CDK9 inhibitor (IC50 = 3.20 nM) with good kinase selectivity. CDK9-IN-29 inhibits cell proliferation and induces apoptosis.
|
-
- HY-108820
-
|
|
HIV Integrase
HIV
|
Infection
|
|
HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 3.7 nM.
|
-
- HY-108817
-
|
|
HIV Integrase
HIV
|
Infection
|
|
HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.
|
-
- HY-139686
-
-
- HY-142487
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 32, an eight membered heterocyclic compound containing N, is a potent KRAS G12C inhibitor.
|
-
- HY-153687
-
|
|
Others
|
Neurological Disease
|
|
SORT-PGRN interaction inhibitor 2 is a SORT-PGRN inhibitor that can decreases SORT1 protein expression and increases extracellular PGRN secretion in mammalian cell lines. SORT-PGRN interaction inhibitor 2 can be used for neurological disease research.
|
-
- HY-153436
-
|
|
RIP kinase
|
Cancer
|
|
RIP1 kinase inhibitor 6 is a potent and selective RIP1 kinase inhibitor with an IC50 of < 100 nM in human R1P1 kinase assay. RIP1 kinase inhibitor 6 is extracted from patent WO2020103884, example 80.
|
-
- HY-N10227
-
-
- HY-151451
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca 2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain.
|
-
- HY-155440
-
|
|
FAK
|
Cancer
|
|
FAK-IN-15 (Compound 9b) is a focal adhesion kinase (FAK) inhibitor with an IC50 value of 0.2691 nM. FAK-IN-15 has anti-tumor activity with an IC50 value of 1.033 μM against U87-MG cells.
|
-
- HY-133014
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders.
|
-
- HY-120300
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase.
|
-
- HY-112131
-
-
- HY-153002
-
-
- HY-130760
-
|
|
HIV Integrase
|
Infection
|
|
HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC50 of 33.3 nM.
|
-
- HY-144639
-
-
- HY-155376
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-14 (compound 14c) is a potent mTOR inhibitor. mTOR inhibitor-14 also shows minimal CYP2C8 inhibition. mTOR inhibitor-14 can inhibit tumor growth.
|
-
- HY-153972
-
|
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
Inflammation/Immunology
|
|
URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia.
|
-
- HY-153437
-
|
|
RIP kinase
|
Cancer
|
|
RIP1 kinase inhibitor 7 (compound 41) is a potent receptor interacting protein 1 kinase (RIP1) Inhibitor with an IC50 of <100 nM for human RIP1. RIP1 kinase inhibitor 7 has an EC50 of 1-100 nM in the cell necrosis assay.
|
-
- HY-12072
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-156799
-
|
|
Cytochrome P450
|
Others
|
|
Cholesterol 24-hydroxylase-IN-2 is an inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), with the IC50 of 5.4 nM. Cholesterol 24-hydroxylase-IN-2 can be used in imaging of cholesterol 24-hydroxylase in mammals.
|
-
- HY-153434
-
|
|
RIP kinase
|
Cancer
|
|
RIP1 kinase inhibitor 4 (Example 3) is a BBB-penetrable RIP1 kinase inhibitor (EC50: <100 nM). RIP1 kinase inhibitor 4 can be used for the research of cell programming necrosis-related diseases. RIP1 kinase inhibitor 4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-152195
-
|
|
Apoptosis
|
Cancer
|
|
ChoKα inhibitor-5 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-5 can inhibit HChoK α1 with an IC50 value of 0.64 μM. ChoKα inhibitor-5 also can induce apoptosis. ChoKα inhibitor-5 can be used for the research of cancer.
|
-
- HY-152191
-
|
|
Apoptosis
|
Cancer
|
|
ChoKα inhibitor-3 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-3 can inhibit HChoK α1 with an IC50 value of 0.66 μM. ChoKα inhibitor-3 also can induce apoptosis. ChoKα inhibitor-3 can be used for the research of cancer.
|
-
- HY-143279
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential.
|
-
- HY-115990
-
|
|
Topoisomerase
Bacterial
|
Infection
|
|
Topoisomerase IV inhibitor 2 (compound 7d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.23 μM and 0.43 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 0.972 μM and 0.608 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
|
-
- HY-115991
-
|
|
Topoisomerase
Bacterial
|
Infection
|
|
Topoisomerase IV inhibitor 2 (compound 5d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.35 μM and 0.55 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 1.985 μM and 0.744 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
|
-
- HY-143906
-
|
|
URAT1
|
Inflammation/Immunology
|
|
URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout.
|
-
- HY-P5943
-
-
- HY-P5942
-
-
- HY-147250A
-
|
RLY-4008 hydrochloride
|
EGFR
|
Cancer
|
|
Lirafugratinib hydrochloride is an orally active selective inhibitor of FGFR2.
|
-
- HY-147250
-
|
RLY-4008
|
EGFR
|
Cancer
|
|
Lirafugratinib is an orally active selective inhibitor of FGFR2.
|
-
- HY-154832
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cav 3.2 inhibitor 4 (compound 21) is a potent, peripherally restricted, selective T-type calcium channel (Cav3.2) inhibitor, with an IC50 of 0.6 μM. Cav 3.2 inhibitor 4 can be used for the research of atrial fibrillation.
|
-
- HY-147134
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 10 (compound 14a) is a highly potent GSK-3β inhibitor with an IC50 value of 80.5 nM. GSK-3β inhibitor 10 can be used for researching Alzheimer’s disease.
|
-
- HY-145436
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-11 (compound 12) is a KRAS inhibitor.
|
-
- HY-116044
-
|
|
Others
|
Neurological Disease
|
|
BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively. BCATc, also called BCAT1, is in the cytoplasm.
|
-
- HY-N3632
-
|
Coronarin D Me ether
|
COX
NF-κB
|
Inflammation/Immunology
|
|
Methoxycoronarin D can be isolated from Hedychium coronarium J. Koenig and is a potent inhibitor of NF-魏B with an IC50 value of 7.3 渭M. Methoxycoronarin D is also a selective inhibitor of COX-1 with an IC50 value of 0.9 渭M.
|
-
- HY-100257
-
-
- HY-143260
-
|
|
GSK-3
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
|
-
- HY-131335
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
|
-
- HY-153968
-
|
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
|
|
URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC50=~10 μM) and Xanthine Oxidase (IC50=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research.
|
-
- HY-115984
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 8 (compound R-13), a benzyl-derivative, is a potent human carbonic anhydrase (hCA) inhibitor with Ki values of 60.7 nM, 320.7 nM, 2298 nM for hCA I, hCA II, hCA IV, respectively.
|
-
- HY-112907
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC50 of 1 nM .
|
-
- HY-12444
-
|
FAK Inhibitor 14
|
FAK
|
Cancer
|
|
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
|
-
- HY-153738
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2.
|
-
- HY-149054
-
|
|
GSK-3
Tau Protein
AAK1
Pim
PKC
|
Neurological Disease
|
|
GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease.
|
-
- HY-155232
-
|
|
Apoptosis
PI3K
|
Cancer
|
|
PI3Kδ-IN-16 is a potent and selective inhibitor of PI3Kδ. PI3Kδ-IN-16 has a strong anti-proliferative effect on cells, causing cell cycle arrest and inducing apoptosis.
|
-
- HY-149311
-
|
|
Others
|
Others
|
|
PPO-IN-2 is an inhibitor of protoporphyrinogen IX oxidase with an Ki of 16 nM.
|
-
- HY-115510
-
|
SPRi3
|
Others
|
Inflammation/Immunology
|
|
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
|
-
- HY-P4306
-
-
- HY-144687
-
|
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
|
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability.
|
-
- HY-19762
-
|
SCD Inhibitor 1
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16.
|
-
- HY-142437
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 8 is a potent ERK inhibitor with an IC50 of 0.48 nM for ERK2 (WO2021110168A1, WX007).
|
-
- HY-148669
-
|
Menin-MLL Inhibitor 24
|
Epigenetic Reader Domain
|
Cancer
|
|
Bleximenib (Menin-MLL inhibitor 24) (compound A) is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor. Bleximenib can be used for the research of cancer.
|
-
- HY-142433
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 7 is a potent ERK inhibitor with an IC50 of 0.94 nM for ERK2 (WO2021110168A1, WX006).
|
-
- HY-150731
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 3 (Compound H5) is a potent Pim-1 kinase inhibitor with an IC50 of 35.13 nM.
|
-
- HY-153807
-
-
- HY-146010
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 13 (compound 7) is a potent carbonic anhydrase (CA) inhibitor, which features 3-methylthiazolo[3,2-a]benzimidazole moiety (as a tail) connected to the zinc anchoring benzenesulfonamide moiety via ureido linker.
|
-
- HY-144641
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 7 (compound 5b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 6.5 nM, 7.1 nM, 72.1 nM, and 255.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively.
|
-
- HY-144640
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 6 (compound 9b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 9.7 nM, 35.2 nM, 88.5 nM, and 91.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively.
|
-
- HY-146391
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
|
-
- HY-120902
-
|
|
GSK-3
|
Inflammation/Immunology
|
|
GSK-3β inhibitor 8, a thiophenacil derivative, is an effective and selective inhibitor of GSK-3β (IC50=64 nM). GSK-3β inhibitor 8 negatively regulated Wnt signaling pathway and stimulated β cell proliferation.
|
-
- HY-141480
-
|
|
GSK-3
Apoptosis
|
Cancer
|
|
GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.
|
-
- HY-151619
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-12 (compound 34) is a sEH inhibitor with an IC50 value of 0.7 μM. sEH inhibitor-12 inhibits the 5-lipoxygenase-activating protein (FLAP)-mediated leukotriene (LT) biosynthesis with an IC50 value of 2.9 μM. sEH inhibitor-12 can be used for the research of inflammation.
|
-
- HY-144686
-
|
|
ATM/ATR
PI3K
mTOR
|
Cancer
|
|
ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC50 of 0.71 nM. ATM Inhibitor-3 shows inhibition of PI3K kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability.
|
-
- HY-131344
-
|
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- HY-151287
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM.
|
-
- HY-153787
-
|
|
ATM/ATR
|
Cancer
|
|
ATM inhibitor-6 (A-193) is a selective ATM kinase inhibitor. ATM inhibitor-6 can be used in cancer research.
|
-
- HY-111409
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04).
|
-
- HY-153199
-
|
|
Others
|
Cancer
|
|
MDM2/XIAP-IN-1 (compound 14) is an orally active inhibitor of dual MDM2/XIAP. MDM2/XIAP-IN-1 has anti-cancer activity with an IC50 value of 0.3 μM, which can be used in cance rescrch.
|
-
- HY-120208
-
-
- HY-114313
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity, with an IC50 value of 9-16 nM in cancer cells.
|
-
- HY-154957
-
|
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC50: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC50s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease.
|
-
- HY-152536
-
|
|
NO Synthase
|
Cancer
|
|
iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells.
|
-
- HY-151617
-
-
- HY-148132
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research.
|
-
- HY-12358
-
|
|
MAP3K
p38 MAPK
MAPKAPK2 (MK2)
|
Cancer
Inflammation/Immunology
|
|
Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers.
|
-
- HY-145022
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3.
|
-
- HY-13973A
-
|
|
GSK-3
|
Metabolic Disease
|
|
GSK-3 inhibitor 1 (compound core 3) is a GSK-3 inhibitor that induces stem/progenitor cell self-renewal (e.g. induces stem/progenitor cell proliferation while maintaining the ability to differentiate into tissue cells in the progeny).
|
-
- HY-156424
-
|
|
Others
|
Inflammation/Immunology
|
|
NOX2-IN-1 (compound 10) is an inhibitor of nicotinamide adenine dinucleotide phosphate oxidase isoform 2 (NOX2). NOX2-IN-1 targets the p47phox−p22phox protein−protein interaction with favorable binding affinities and cellular activities.
|
-
- HY-155311
-
|
|
Others
|
Inflammation/Immunology
|
|
NKG2D-IN-1 (compound 21) is a natural killer group 2D receptor (NKG2D) inhibitor with IC50s of 0.3 µM and 0.7 µM in NKG2D/MICA and ULBP6 TR-FRET assays, respectively.
|
-
- HY-155153
-
|
|
CDK
Apoptosis
|
Others
|
|
CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research.
|
-
- HY-15736
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
|
-
- HY-153760
-
-
- HY-148261
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 56 (compound IC-6) is a potent SOS1 inhibitor with an IC50 of 1.6 nM. KRAS G12C inhibitor 56 can be used in cancer research.
|
-
- HY-136728
-
|
|
Caspase
|
Cancer
|
|
Ac-YVAD-AOM is the inhibitor of caspase-1 that shows antitumor activity.
|
-
- HY-154958
-
|
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases.
|
-
- HY-139607
-
|
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
SSAO inhibitor-1 is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor. SSAO inhibitor-1 has anti-inflammatory activity and can be used for liver diseases research.
|
-
- HY-139894
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential research of pancreatic cancer.
|
-
- HY-139885
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 4 is a potent, orally bioavailable c-MYC-reducing compound.
|
-
- HY-143261
-
|
|
GSK-3
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC50 value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
|
-
- HY-150963
-
|
|
Renin
|
Cardiovascular Disease
|
|
Renin inhibitor-1 (compound 26) is a potent and orally active renin inhibitor with IC50s of 0.9, 1.8 nM for rh-renin and hPRA, respectively. Renin inhibitor-1 shows antihypertensive efficacy. Renin inhibitor-1 has the potential for the research of hypertension and cardiovascular/renal diseases.
|
-
- HY-147374
-
|
|
Epigenetic Reader Domain
|
Metabolic Disease
Inflammation/Immunology
|
|
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases.
|
-
- HY-148317
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor. PI3Kγ inhibitor 6 can be used for the research of inflammatory and autoimmune diseases.
|
-
- HY-18353
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-151288
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC50 value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research.
|
-
- HY-W412264
-
|
|
Pim
|
Cancer
|
|
Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer.
|
-
- HY-19761
-
|
|
RIP kinase
|
Cancer
|
|
RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
|
-
- HY-10247
-
|
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-P5542
-
-
- HY-137497
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-142834
-
-
- HY-10885
-
|
ABT-472
|
PARP
|
Cancer
|
|
A-620223 (succinate) (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 (succinate) (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research.
|
-
- HY-142478
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 29 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 3. KRAS G12C inhibitor 29 can be used for the research of cancer.
|
-
- HY-142481
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer.
|
-
- HY-142485
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 31 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer.
|
-
- HY-142490
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 33 is a KRAS G12C inhibitor extracted from patent WO2021244603A1, compound 1. KRAS G12C inhibitor 33 can be used for the research of cancer.
|
-
- HY-155211
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC50 of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC50 of 119 nM.
|
-
- HY-147375
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40.
|
-
- HY-153461
-
|
|
Ras
|
Cancer
|
KRAS G12C inhibitor 58 is a KRAS G12C inhibitor, used in cancer research.
|
-
- HY-156966
-
|
|
Autophagy
|
Cancer
|
|
ATG12-ATG3 inhibitor 1 (compound 189) is a potent inhibitor of autophage.
|
-
- HY-12860
-
|
Notch Inhibitor 1
|
Notch
|
Cancer
|
|
BMS-986115 (Notch inhibitor 1) is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer.
|
-
- HY-151616
-
|
|
Epoxide Hydrolase
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
sEH inhibitor-10 (Compound 37) is a selective soluble epoxide hydrolase (sEH) inhibitor (IC50=0.5 μM). sEH inhibitor-10 maintains high cycloeicosatrienoic acid (EETs) levels by inhibiting sEH, thereby reducing inflammation, regulating endothelial tone, improving mitochondrial function, and reducing oxidative stress. sEH inhibitor-10 has good research potential in metabolic, renal and cardiovascular diseases.
|
-
- HY-122914
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf.
|
-
- HY-153944
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 60 (compound 23) is a Kras-G12C inhibitor. KRAS G12C inhibitor 60 can be used for the research of lung cancer, colorectal cancer, pancreatic cancer.
|
-
- HY-142511
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 34 is a KRAS G12C inhibitor extracted from patent WO2021239058A1, compound Z1. KRAS G12C inhibitor 34 can be used for the research of cancer.
|
-
- HY-143294
-
|
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
sEH inhibitor-2 (compound 5l) is an orally active (predicted percentage absorption: 71.2-88.4%) soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 0.9 nM. sEH inhibitor-2 can maintain epoxyeicosatrienoic acids (EETs) serum level in high concentrations. sEH inhibitor-2 can be used in study of cardiovascular protection.
|
-
- HY-149309
-
|
|
Topoisomerase
|
Infection
|
|
Topoisomerase inhibitor 2 (18C) is a bacterial topoisomeraseinhibitor that exhibits potent broad-spectrum activity against multidrug-resistant Gram-negative bacteria.
|
-
- HY-101282
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.
|
-
- HY-145843
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes.
|
-
- HY-151599
-
|
|
Bacterial
|
Infection
|
|
Pks13-TE inhibitor 3 (compound 23) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.55 μM). Pks13-TE inhibitor 3 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistant Mtb strains (MIC=0.0625-0.25 μg/mL). Pks13-TE inhibitor 3 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB.
|
-
- HY-151598
-
|
|
Bacterial
|
Infection
|
|
Pks13-TE inhibitor 2 (compound 32) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.30 μM). Pks13-TE inhibitor 2 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistant Mtb strains (MIC=0.0039-0.0078 μg/mL). Pks13-TE inhibitor 2 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB.
|
-
- HY-150003
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC50 value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease.
|
-
- HY-P1408A
-
|
|
Integrin
|
Cancer
|
|
Obtustatin triacetate is a 41-residue non-RGD disintegrin. Obtustatin triacetate can be isolated from the venom of Vipera lebetina obtusa. Obtustatin triacetate is a potent and selective inhibitor of integrin α1β1 adhesion to type IV collagen. Obtustatin triacetate inhibits angiogenesis and may be used in cancer research.
|
-
- HY-157138
-
|
|
Others
|
Cancer
|
|
MMP-9-IN-8 (Compound 3) is an MMP-9 inhibitor with inhibitory activities of 42.16% and 58.28% at 10 μM and 50 μM concentrations, respectively. MMP-9-IN-8 has anti-cancer activity and can induce apoptosis in MCF-7 cells with an IC50 value of 23.42 μM.
|
-
- HY-103268
-
|
|
Potassium Channel
|
Neurological Disease
|
|
(Rac)-AZD3839 is an orally active beta-amyloid precursor protein cleaving enzyme (BACE1) inhibitor that is blood-brain barrier-permeable. (Rac)-AZD3839 has an affinity for the human ether-a-go-go related gene (hERG) ion channel. (Rac)-AZD3839 can be used in the research of Alzheimer's disease.
|
-
- HY-155350
-
|
|
Microtubule/Tubulin
|
Others
|
|
Tubulin polymerization-IN-53 (compound 4b) is an inhibitor of β-tubulin polymerization. Tubulin polymerization-IN-53 can arrest the cell cycle at the G2/M stage. Tubulin polymerization-IN-53 has antiproliferative efficacy against the MDA-MB-231 cell line with an IC50 value of 3.24 μM.
|
-
- HY-156410
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-23 (compound 15) is an inhibitor of JFMS-like tyrosine kinase 3 (FLT3) with an IC50 of 7.42 nM. FLT3-IN-23 has antiproliferative activities against BaF3 cells carrying various FLT3-TKD and FLT3-ITD-TKD mutations.
|
-
- HY-139629
-
-
- HY-139648
-
-
- HY-139206
-
-
- HY-148573
-
-
- HY-111370
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
|
-
- HY-144708
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC50 of 28.8 μM.
|
-
- HY-123322
-
-
- HY-P2949
-
|
|
Potassium Channel
|
Cancer
|
|
Pandinotoxin Kα, isolated from the venom of Pandinus imperator, is the inhibitor of A-type potassium channel.
|
-
- HY-147388
-
|
|
Others
|
Metabolic Disease
|
|
hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea.
|
-
- HY-17602
-
|
BBI503
|
Others
|
Cancer
|
|
Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitory activity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
|
-
- HY-101275
-
-
- HY-149996
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 6 (Compound 4d) is a potent Pim-1 kinase inhibitor with IC50 value of 0.46 μM, and has significant cytotoxic effect on cancer cells.
|
-
- HY-13277
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
|
-
- HY-15886
-
|
Mitochondrial division Inhibitor 1
|
Dynamin
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. Mdivi-1 is a mitochondrial division/mitophagy inhibitor.
|
-
- HY-15288
-
|
|
PI3K
|
Cancer
|
|
PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
|
-
- HY-W018931
-
|
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.
|
-
- HY-149995
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 5 (Compound 4c) is a Pim-1 kinase inhibitor (IC50: 0.61 μM). Pim-1 kinase inhibitor 5 shows cytotoxicity against cancer cells, with IC50s of 6.95-20.19 μM for HepG2, MCF-7, PC3, and HCT-116 cells.
|
-
- HY-112616
-
|
|
NAMPT
Drug-Linker Conjugates for ADC
|
Cancer
|
|
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
|
-
- HY-155151
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC50 values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC50 value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay.
|
-
- HY-163004
-
|
|
Trk Receptor
|
Cancer
|
|
Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers.
|
-
- HY-148787
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
Oditrasertib is a RIPKl inhibitor with an IC50 value lower than 100 nM. Oditrasertib can be used for the research of Inflammation.
|
-
- HY-121879
-
SHP836
1 Publications Verification
|
SHP2
Phosphatase
|
Cancer
|
|
SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
|
-
- HY-121935
-
|
|
Fungal
|
Infection
|
|
Tecnazene (2,3,5,6-Tetrachloronitrobenzene) is a fungicide and is used as a sprout inhibitor on stored potatoes.
|
-
- HY-P5955
-
|
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity.
|
-
- HY-149699
-
-
- HY-P5938
-
|
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable caspase-1 inhibitor that has antitumor activity.
|
-
- HY-111412
-
-
- HY-112287
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.
|
-
- HY-101766
-
|
BGB-3111 analog
|
Btk
|
Inflammation/Immunology
|
|
Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
|
-
- HY-112494
-
|
|
Ras
|
Cancer
|
|
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
|
-
- HY-112491
-
|
|
Ras
|
Cancer
|
|
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
|
-
- HY-132979
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities.
|
-
- HY-147631
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 50 (Example 4) is a KRAS G12C inhibitor with an IC50 of 46.7 nM.
|
-
- HY-112493
-
|
|
Ras
|
Cancer
|
|
KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
|
-
- HY-15223
-
MI-3
1 Publications Verification
Menin-MLL Inhibitor 3
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC50 of 648 nM and a Kd of 201 nM.
|
-
- HY-112492
-
|
|
Ras
|
Cancer
|
|
KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
|
-
- HY-145017
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 20 is a KRAS G12C inhibitor extracted from patent CN112694475A, example 1.
|
-
- HY-124594
-
|
GS-6207 analog
|
HIV
|
Infection
|
|
CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition. CA inhibitor 1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-156549
-
|
|
ERK
Ras
|
Cancer
|
|
KRAS G12C inhibitor 61 (Example 3) inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. KRAS G12C inhibitor 61 can be used for research of pancreatic, colorectal, and lung cancers.
|
-
- HY-139605
-
|
|
GLUT
|
Cancer
Inflammation/Immunology
|
|
GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases.
|
-
- HY-P4136
-
|
|
ERK
|
Cancer
|
|
Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM.
|
-
- HY-146543
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-146533
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-146545
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-15 (compound 3-19) is a potent KRAS G12C inhibitor with an IC50 of 0.954 µM. KRAS inhibitor-15 shows p-ERK inhibition activities with IC50s of 2.03, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-15 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-146476
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-146546
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-138295
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 (compound 11) selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
|
-
- HY-146475
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC50 of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC50s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-146544
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-112615
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
|
-
- HY-112914
-
|
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.
|
-
- HY-144685
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-2 (compound 7) is a potent and selective ATM inhibitor, with an IC50 of <1 nM.
|
-
- HY-130260
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents.
|
-
- HY-128703
-
-
- HY-147668
-
|
|
Others
|
Neurological Disease
|
|
α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4%.
|
-
- HY-147666
-
|
|
Others
|
Neurological Disease
|
|
α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2%.
|
-
- HY-147669
-
|
|
Others
|
Neurological Disease
|
|
α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8%.
|
-
- HY-126144
-
|
|
GSK-3
|
Metabolic Disease
|
|
GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.
|
-
- HY-147667
-
|
|
Others
|
Neurological Disease
|
|
α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3%.
|
-
- HY-112807
-
|
|
SGLT
|
Metabolic Disease
|
|
SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
|
-
- HY-142946
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo.
|
-
- HY-157167
-
|
|
mTOR
|
Cancer
Neurological Disease
|
|
mTORC1-IN-1 (T1) is a rapamycin homologue (rapalog) and selective mTORC1 inhibitor. mTORC1-IN-1 regulates cell growth and metabolism and is implicated in a variety of diseases including cancer. mTORC1-IN-1 targets mTORC1 by binding to the FKBP12-FRB complex (docking score = −11.6 kcal/mol).
|
-
- HY-157067
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 62 is a KRAS G12C inhibitor. KRAS G12C inhibitor 62 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1).
|
-
- HY-145018
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 21 is a KRAS G12C inhibitor extracted from patent WO2021219090A1, example 7.
|
-
- HY-153899
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 59 is a KRAS G12C inhibitor with anticancer effects (WO2023036282A1, compound II).
|
-
- HY-126292
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.
|
-
- HY-145019
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 22 is a KRAS G12C inhibitor extracted from patent WO2021219072A1, example 120.
|
-
- HY-139911
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 7 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683, compound 114) .
|
-
- HY-156393
-
|
|
ERK
|
Cancer
|
|
Laxiflorin B, a herbal compound, is a novel selective ERK1/2 inhibitor that has antitumor activity.
|
-
- HY-124556
-
|
|
Elastase
|
Inflammation/Immunology
|
|
Elasnin is a selective granulocyte elastase inhibitor. Elasnin is almost ineffective for pancreatic elastase, trypsin, chymotrypsin, thermolysin and papain.
|
-
- HY-128859
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
|
-
- HY-32015
-
|
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-153668
-
-
- HY-151452
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Cav 3.2 inhibitor 3 (Compound 4) is a potent Cav3.2 T-type Ca 2+ channel inhibitor with an IC50 of 0.1534 μM, and has little binding affinity to D2 receptors.
|
-
- HY-17541A
-
|
|
Cathepsin
|
Others
|
|
Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
|
-
- HY-17541
-
|
|
Cathepsin
|
Others
|
|
Cysteine Protease inhibitor is an inhibitor of cysteine protease.
|
-
- HY-132299
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation.
|
-
- HY-146226
-
|
|
Enterovirus
|
Infection
|
|
Viral 2C protein inhibitor 1 (compound 6aw) is a potent and broad-spectrum enterovirus antiviral agent, inhibiting viral 2C protein. Viral 2C protein inhibitor 1 inhibits multiple strains of EV-D68, EV-A71 and CVB3 with EC50s of 0.1~3.6 µM, and exhibits high selectivity index and relatively low cytotoxicity.
|
-
- HY-153753
-
|
|
Others
|
Cancer
|
|
Wnt pathway inhibitor 4 (compound 16D) is an anticancer agent that has anti-proliferative activity.
|
-
- HY-112335
-
|
|
Src
Interleukin Related
|
Cancer
|
|
Lck Inhibitor III (compound 12h) is a potent Lck inhibitor, with an IC50 of 867 nM. Lck Inhibitor III inhibits IL-2 synthesis in Jurkat cells, with an IC50 of 1.270 μM.
|
-
- HY-114168
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147.
|
-
- HY-139910
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 6 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683A1, compound 112) .
|
-
- HY-139880
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.
|
-
- HY-151523
-
|
|
Ras
|
Cancer
|
|
KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research.
|
-
- HY-B0331
-
-
- HY-148742
-
|
|
RET
|
Cancer
|
|
RET-IN-21 is an inhibitor of receptor tyrosine kinase (RET), with the IC 50 of 4.4 μM, that has antitumor activity.
|
-
- HY-120248
-
|
|
Adenosine Deaminase
|
Cancer
|
|
FR221647 is an orally active non-nucleoside inhibitor of adenosine deaminase. FR221647 is not cytotoxic at a concentration of 100 μM.
|
-
- HY-B0331B
-
-
- HY-P2785
-
-
- HY-152193
-
|
|
Others
|
Cancer
|
|
ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression.
|
-
- HY-145025
-
|
|
ERK
|
Cancer
Inflammation/Immunology
|
|
ERK1/2 inhibitor 3 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 3 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021218912A1, compound 1).
|
-
- HY-145026
-
|
|
ERK
|
Cancer
Inflammation/Immunology
|
|
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1).
|
-
- HY-145027
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 5 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2020238776A1).
|
-
- HY-145028
-
|
|
ERK
|
Cancer
Inflammation/Immunology
|
|
ERK1/2 inhibitor 6 is a potent inhibitor of ERK1/2. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of the MAPK family. ERK1/2 inhibitor 6 has the potential for the research or prevention of cancer, inflammation or other proliferative diseases (extracted from patent WO2021063335A1, compound 1).
|
-
- HY-153937
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Skp2 inhibitor 2 (14f) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC50 value of 10.2 μM (Skp2-Cks1). Skp2 is a part of cullin-RING ligases, which recruits and ubiquitinates substrates, involving in proteolytic and non-proteolytic process.
|
-
- HY-112601
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. Anticancer activity.
|
-
- HY-10421
-
|
|
c-Met/HGFR
|
Cancer
|
|
Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor.
|
-
- HY-148000
-
-
- HY-151621
-
-
- HY-155091
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-9 (Compd 7a) is a potent ATM inhibitor with IC505 nM for ATM kinase, useful in cancer research.
|
-
- HY-153412
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-22 (compound FB9/6B9) is a potent inhibitor of K-Ras. KRAS inhibitor-22 targets to Kras 4B(G12D) and (G12C), which can be used for cancer research.
|
-
- HY-112505
-
|
|
BCRP
|
Cancer
|
|
Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively.
|
-
- HY-112390A
-
|
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-112390
-
|
|
5-HT Receptor
Syk
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-156672
-
|
|
FGFR
|
Cancer
|
|
S6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC50: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC50: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes.
|
-
- HY-126144A
-
|
|
GSK-3
|
Metabolic Disease
|
|
(E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers. GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.
|
-
- HY-146537
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-147595
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 15 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243). KRAS G12D inhibitor 15 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-155968
-
|
|
HBV
|
Infection
|
|
HBV-IN-40 (Compound 11826096) is a HBV inhibitor (IC50: 0.7 μM). HBV-IN-40 is an antiviral agent.
|
-
- HY-155351
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-15 (Compound 18) is a PARP7 inhibitor with IC50 of 0.56 nM, that has antitumor activity.
|
-
- HY-148138
-
|
|
HIV
|
Infection
|
|
Deaminase inhibitor-1 is a small molecule inhibitor of APOBEC3G DNA Deaminase, with an IC50 value of 18.9 μM.
|
-
- HY-148535
-
|
|
Proteasome
|
Neurological Disease
|
|
Calpain Inhibitor XI is a reversible covalent inhibitor of calpain-1. Calpain Inhibitor XI can be used for the research of neurodegenerative disorders.
|
-
- HY-119937
-
-
- HY-146194
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin。NHEJ inhibitor-1 also induces ROS generation and MMP deduction.
|
-
- HY-32018
-
|
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-146807
-
|
|
Trk Receptor
|
Cancer
|
|
Type II TRK?inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK?inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively. Type II TRK?inhibitor 1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149411
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
Inflammation/Immunology
|
|
IDO1/TDO-IN-6 (compound 11) is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively. IDO1/TDO-IN-6 has inhibitory effects on IDO1 and TDO, with Ki values of 1.9 and 3.1 μM, respectively. IDO1/TDO-IN-6 can be used in cancer and immunology research.
|
-
- HY-135864
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
|
-
- HY-135866
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
|
-
- HY-147733
-
-
- HY-146643
-
-
- HY-135865
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
|
-
- HY-70003
-
|
CPG2 Inhibitor
|
Carboxypeptidase
|
Cancer
|
|
Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
|
-
- HY-156818
-
|
|
Others
|
Cancer
|
|
TNIK-IN-7 (Compound 8) is an inhibitor of Traf2 and Nck-interacting kinase (TNIK), with IC50 of 11 nM, that has antitumor activity.
|
-
- HY-155341
-
|
|
FLT3
|
Cancer
|
|
HSK205 is a dual FLT3 and haspin inhibitor, with IC50 of 0.187 nM for FLT3. HSK205 has antitumor activity.
|
-
- HY-124762
-
|
|
Others
|
Cancer
|
|
TNIK-IN-1 (Compound 1) is an inhibitor of Traf2 and Nck-interacting kinase (TNIK), with IC50 of 65 nM, that has antitumor activity.
|
-
- HY-155945
-
|
|
Others
|
Others
|
|
Firefly luciferase-IN-1 (compound 48) is a highly potent and reversible inhibitor of firefly luciferase with an IC50 value of 0.25 nM.
|
-
- HY-130673
-
|
|
NO Synthase
|
Cardiovascular Disease
|
|
L-NABE is a nitric oxide (NO) synthase inhibitor. L-NABE is also a potent endothelium dependent vasoconstrictor and inhibitor of relaxation.
|
-
- HY-126388
-
-
- HY-P5786
-
-
- HY-151968
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis.
|
-
- HY-142945
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively.
|
-
- HY-155058
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Nav1.3 channel inhibitor 1 (compound 15b) is a state-dependent voltage-gated sodium channel Nav1.3 inhibitor (IC50=20 nM). Nav1.3 channel inhibitor 1 can penetrate the blood-brain barrier and can be used in the research of nervous system diseases.
|
-
- HY-77048
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM. IRAK-4 protein kinase inhibitor 2 can be used for the research of inflammatory and immune-related conditions or disorders.
|
-
- HY-149648
-
|
|
RSV
|
Infection
|
|
JNJ-8003 is a potent inhibitor of RSV Polymerase. JNJ-8003 inhibits nucleotide polymerization of RNA transcription and replication at the early stages.
|
-
- HY-148260
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 16 is a KRAS G12D inhibitor. KRAS G12D inhibitor 16 has inhibitory activity against KRAS G12D and KRAS G12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC).
|
-
- HY-112286
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
|
-
- HY-112439
-
-
- HY-111451
-
|
M1774; ATR Inhibitor 1
|
ATM/ATR
|
Cancer
|
|
Tuvusertib (M1774; ATR inhibitor 1) is a selective and orally active ATR inhibitor extracted from patent WO2015187451A1, compound I-l, with a Ki value below 1 μΜ.
|
-
- HY-110156
-
|
|
Others
|
Cancer
|
|
Y29 is a potent PFKFB3 inhibitor with an IC50 of 0.183 µM, and acts as a competitive inhibitor against Fru-6-P with a Ki of 0.094 µM. Y29 also inhibits the HeLa cell growth with a GI50 of 2.7 µM.
|
-
- HY-151197
-
|
|
HIV Protease
|
Infection
|
|
HIV protease-IN-1 (compound 1·succinate) is a potent HIV protease non-peptidic inhibitor, can be used to research AIDS.
|
-
- HY-103526
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DPNI-GABA is a nitroindoline cage compound that inhibits GABA(A) receptors and reduces GABA-evoked peak responses with an IC50 value of 0.5 mM.
|
-
- HY-15167
-
|
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
|
-
- HY-142655
-
-
- HY-143592
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494).
|
-
- HY-144661
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.
|
-
- HY-125873
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM.
|
-
- HY-125875
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM.
|
-
- HY-125874
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM.
|
-
- HY-125872
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 17, has an IC50 of 18 nM.
|
-
- HY-110247
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
|
TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
|
-
- HY-142706
-
|
|
Monoamine Oxidase
HDAC
|
Cancer
|
|
MAO A/HDAC-IN-1 is a dual inhibitor of monoamine oxidase A (MAO A) and HDAC. MAO A/HDAC-IN-1 can be used for glioma research.
|
-
- HY-157154
-
|
|
SARS-CoV
|
Infection
|
|
MAT-POS-e194df51-1 is an orally active, non-covalent and non-peptide SARS-CoV-2 main protease (M pro) inhibitor with an IC50 value of 37nM. MAT-POS-e194df51-1 is cytotoxic with EC50 values of 64 nM and 126 nM in A549-ACE2-TMPRSS2 cells and HeLa -ACE2 cells, respectively.
|
-
- HY-151577
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.
|
-
- HY-113844
-
|
|
Ser/Thr Protease
|
Others
|
|
Ac-Gly-Lys-OMe is a substrate for urokinase. Ac-Gly-Lys-OMe can be used to measure the effects of small molecule inhibitors on urokinase activity.
|
-
- HY-10249A
-
|
|
Akt
|
Cancer
|
|
AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
|
-
- HY-143588
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 35 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 35 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent CN112920183A, compound 3).
|
-
- HY-156019
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-10 (Compound 4i) is an FGFR1 inhibitor (IC50: 28 nM). FGFR1 inhibitor-10 inhibits the phosphorylation of FGFR1. FGFR1 inhibitor-10 has anti-angiogenic, anti-invasion activity, and anti-tumor effect.
|
-
- HY-12446
-
|
|
Ras
|
Cancer
|
|
K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C).
|
-
- HY-129166
-
|
|
Bacterial
|
Infection
|
|
UCM53, a FtsZ inhibitor, is an antibacterial agent. UCM53 can inhibit the growth of clinical isolates of antibiotic-resistant Staphylococcus aureus and Enterococcus faecalis
|
-
- HY-130011
-
-
- HY-139630
-
-
- HY-149654
-
-
- HY-N3267
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Methyl pseudolarate B, a natural diterpenoid, is a protein tyrosine phosphatase 1B (PTP1B) (Phosphatase) inhibitor with an IC50 value of 10.9 μM.
|
-
- HY-143590
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 37 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 37 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2018143315A1, compound 65).
|
-
- HY-143606
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 12 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 134).
|
-
- HY-143594
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 40 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 40 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 70).
|
-
- HY-134811
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 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-146061
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively.
|
-
- HY-143604
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 11 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 52).
|
-
- HY-143591
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 38 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 38 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129820A1, compound 171).
|
-
- HY-143598
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 42 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 42 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2020146613A1, compound 10).
|
-
- HY-143599
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 8 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 8 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021107160A1, compound 2).
|
-
- HY-143607
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142).
|
-
- HY-143602
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20).
|
-
- HY-143596
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 41 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 41 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 121).
|
-
- HY-143603
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 10 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 10 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 34).
|
-
- HY-147322
-
|
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC50 value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity.
|
-
- HY-15679
-
|
|
PI4K
|
Cancer
|
|
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
|
-
- HY-149681
-
|
|
Beclin1
Bcl-2 Family
|
Cancer
|
|
Beclin1-Bcl-2 interaction inhibitor 1 potently inhibits Beclin 1/Bcl-2 binding. Beclin1-Bcl-2 interaction inhibitor 1 can be used for the research of cancer and neurodegeneration.
|
-
- HY-120494
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-1 (compound TCPU ) is a potent and oral active inhibitor of sEH (soluble epoxide hydrolase) with IC50s of 0.4 and 5.3 nM in human and murine, respectively.
|
-
- HY-115753
-
|
|
Proteasome
|
Neurological Disease
|
|
Calpain Inhibitor-1 (compound 36) is a potent and selective cysteine protease calpain 1 (Cal1) inhibitor (IC50=100 nM; Ki=2.89 μM).
|
-
- HY-155195
-
|
|
Others
|
Cancer
|
|
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.
|
-
- HY-W181102
-
|
|
Others
|
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17).
|
-
- HY-149488
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor (IC50s: 0.85 nM). FGFR1 inhibitor-9 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-9 has anticancer activity.
|
-
- HY-149487
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-8 (Compound 9) is a FGFR1 inhibitor (IC50s: 0.5 nM). FGFR1 inhibitor-8 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-8 has anticancer activity.
|
-
- HY-18707
-
|
|
Ras
Apoptosis
|
Cancer
|
|
K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.
|
-
- HY-144987
-
|
|
CD38
|
Cancer
|
|
RBN013209 is a potent CD38 inhibitor with an IC50 of 0.01-0.1 μM for human CD38. RBN013209 can be used for the research of of cancer.
|
-
- HY-117368
-
|
(2R)-AL-5898
|
COX
|
Inflammation/Immunology
|
|
AL-8417 ((2R)-AL-5898) is a potent inhibitor of Cyclooxygenase (COX), with IC50 of 120 μM, that plays an important role in inflammatory response.
|
-
- HY-N1159
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Teuclatriol is an NF-κB inhibitor can be isolated from salvia mirzayanii, has anti-inflammatory effects. Teuclatriol inhibits TNF-α secretion in a dose-dependent manner.
|
-
- HY-148669A
-
|
Menin-MLL Inhibitor 24 oxalate
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 24 (compound A) oxalate is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor, and can be used for the research of cancer.
|
-
- HY-156875
-
-
- HY-P1111
-
|
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-139624
-
|
|
JNK
|
Others
|
|
JNK3 inhibitor-1 is a potent and selective JNK3 inhibitor (IC50 = 0.005 μM). JNK3 inhibitor-1 is orally bioavailable and brain penetrant.
|
-
- HY-13984
-
|
|
EGFR
|
Cancer
|
|
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
|
-
- HY-149866
-
|
|
Reverse Transcriptase
HIV
Cytochrome P450
|
Infection
|
|
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch.
|
-
- HY-146617
-
|
|
Glutaminase
Apoptosis
|
Cancer
|
|
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity.
|
-
- HY-N10686
-
|
|
Cholinesterase (ChE)
|
Cancer
|
|
Tanshinone IIA anhydride is a potent and irreversible human carboxylesterase (CE) inhibitor with Ki values of 1.9 nM and 1.4 nM for human CE1 and the human intestinal CE (hiCE), respectively.
|
-
- HY-12315
-
|
N-Oxaloglycine
|
Others
|
Cancer
|
|
N-Oxalylglycine (N-Oxaloglycine) is a broad-spectrum 2-oxoglutarate oxygenase inhibitor. N-Oxalylglycine can be used in studies on the hypoxic response and chromatin modifications in animals.
|
-
- HY-107841
-
|
|
Ras
|
Cancer
|
|
K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C).
|
-
- HY-149693
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-11 (compound 25) is an inhibitor of Aurora Kinase with an IC50 of 0.14 μM. Aurora kinase inhibitor-11 has anticancer activity.
|
-
- HY-152209
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC50 values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer.
|
-
- HY-112605
-
|
|
Phospholipase
|
Cardiovascular Disease
|
|
sPLA2-X Inhibitor 31 is a selective secreted phospholipase A2 type X (sPLA2-X) inhibitor with IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively.
|
-
- HY-146616
-
|
|
Glutaminase
|
Cancer
|
|
GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity.
|
-
- HY-147993
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity.
|
-
- HY-153433
-
|
|
Others
|
Neurological Disease
|
|
Serine Hydrolase inhibitor-21 (compound 8), a pyridine, is a serine hydrolase inhibitor with a Ki of 429 nM for BuChE. Serine Hydrolase inhibitor-21 has the potential for Alzheimer's disease research.
|
-
- HY-146088
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-31 (compound 4) is a potent HIV-1 inhibitor. HIV-1 inhibitor-31 can be used for researching AIDS.
|
-
- HY-115900
-
|
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 4 (compound 16), a mandelic acid-based spirothiazolidinone, has potent antimycobacterial activity against Mycobacterium tuberculosis strain H37Rv with the high inhibition value 98% at lower than 6.25 µg/mL concentration.
|
-
- HY-111752
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
|
-
- HY-153930
-
-
- HY-145909
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.
|
-
- HY-143272
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase.
|
-
- HY-142468
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-12 is potent HIV-1 inhibitor. HIV-1 inhibitor-12 inhibits HIV-1 capsid protein polymerization with an IC50 of 9 nM (WO2021104413A1, compound 1-1a).
|
-
- HY-N12133
-
|
|
Others
|
Metabolic Disease
|
|
4,7-Didehydroneophysalin B is a flavonoid with cholinesterase inhibiting activity. 4,7-Didehydroneophysalin B can be isolated and purified from the natural Physalis alkekengi L. var. franchetii (Mast.) Makino.
|
-
- HY-149476
-
|
|
Lipoxygenase
|
Neurological Disease
|
|
5-LOX-IN-5 (Compound 29) is a 5-LOX inhibitor (IC50: 56 nM). 5-LOX-IN-5 can be used for research of neurodegenerative diseases.
|
-
- HY-141525
-
-
- HY-112812
-
-
- HY-144991
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.
|
-
- HY-112851
-
-
- HY-15535
-
DMAT
3 Publications Verification
CK2 Inhibitor; Casein kinase II Inhibitor
|
Casein Kinase
|
Cancer
|
|
DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
|
-
- HY-149519
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity.
|
-
- HY-146660
-
|
|
c-Myc
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity.
|
-
- HY-146208
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.
|
-
- HY-10549
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
|
-
- HY-142444
-
|
|
AP-1
|
Metabolic Disease
|
|
SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).
|
-
- HY-151962
-
|
|
JNK
Apoptosis
GSK-3
p38 MAPK
|
Neurological Disease
|
|
JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable.
|
-
- HY-156790
-
|
|
FGFR
|
Cancer
|
|
FGFR3-IN-6 is a potent and selective FGFR3 inhibitor with IC50 value less than 350 nM. FGFR3-IN-6 can be used in research of cancer.
|
-
- HY-P10093
-
|
|
PI3K
|
Others
|
|
Penetratin-PI3Kγ(126-150) is a peptide inhibitor of ΡI3Κγ that plays an important role in respiratory system diseases.
|
-
- HY-156791
-
|
|
FGFR
|
Cancer
|
|
FGFR3-IN-7 is a potent and selective FGFR3 inhibitor with IC50 value less than 350 nM. FGFR3-IN-7 can be used in research of cancer.
|
-
- HY-112374
-
|
|
Others
|
Neurological Disease
|
|
NPAS3-IN-1 is a potent inhibitor of NPAS3-ARNT heterodimerization and regulates NPAS3 transcription by disrupting the heterodimerization of NPAS3 with ARNT at the cellular level.
|
-
- HY-112911
-
-
- HY-152200
-
|
|
HIV Protease
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS).
|
-
- HY-148043
-
|
|
Others
|
Others
|
|
Schnurri-3 inhibitor-1 is a potent schnurri-3 inhibitor which is an essential regulator of adult bone formation. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL with an AC50 value of 2.09 μM. Schnurri-3 inhibitor-1 can be used to research osteoporosis.
|
-
- HY-10249D
-
|
|
Akt
|
Cancer
|
|
AKT Kinase Inhibitor hydrochloride is an Akt kinase inhibitor with anti-tumor activity. AKT Kinase Inhibitor (hydrochloride) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146308
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS.
|
-
- HY-112373
-
|
|
Aurora Kinase
|
Others
|
|
Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket.
|
-
- HY-147750
-
|
|
Phosphodiesterase (PDE)
|
Cancer
Neurological Disease
|
|
TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC50 of 3.5 μM.
|
-
- HY-P5982
-
|
|
Phosphatase
|
Neurological Disease
|
|
PTPσ Inhibitor, ISP can bind to recombinant human PTPs and inhibits PTPσ signaling. PTPσ Inhibitor, ISP can penetrate the membrane and relieves the chondroitin sulfate proteoglycan (CSPG)-mediated axonal sprouting inhibition in spinal cord injury model. PTPσ Inhibitor, ISP enhances remyelination in LPC-induced demyelinated spinal cord. PTPσ Inhibitor, ISP also promotes oligodendrocyte progenitor cells (OPCs) migration, maturation, remyelination, and functional recovery in animal models of Multiple Sclerosis (MS).
|
-
- HY-112478
-
|
|
Phosphatase
SHP2
|
Cancer
|
|
PTP Inhibitor IV is a protein tyrosine phosphatase (PTP) inhibitor that competitively inhibits DUSP14 phosphatase activity with an 50 of 5.21 μM. PTP Inhibitor IV inhibits SHP-2, PTP1B, PTP-ε, PTP Meg-2, PTP-σ, PTP-β, and PTP-μ with 50s of 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively.
|
-
- HY-153703
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity. PI3Kγ inhibitor 7 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-142253
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-10 is a nanomolar HIV-1 maturation inhibitor.
|
-
- HY-149260
-
-
- HY-14829F
-
|
5-epi-Isofagomine
|
Glucosidase
|
Metabolic Disease
|
|
L-Afegostat (5-epi-Isofagomine) is a glycosidase inhibitor. L-Afegostat is an iminosugar that can be used for the synthesis of carbohydrates. L-Afegostat shows enzyme inhibition to β-Glucosidase with an Ki of 30 μM.
|
-
- HY-147229
-
|
|
Ras
|
Cancer
|
|
GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research.
|
-
- HY-152560
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC50 value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection.
|
-
- HY-21141
-
|
|
Cathepsin
|
Cancer
|
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-149268
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-6 (Compound A53) is a selective JNK3 Inhibitor (IC50=78 nM). JNK3 inhibitor-6 has neuroprotective effect, and can used for research of neurodegenerative diseases.
|
-
- HY-148395
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
UCK2 Inhibitor-2 is a non-competitive uridine-cytidine kinase 2 (UCK2) inhibitor with an IC50 value of 3.8 µM. UCK2 Inhibitor-2 can suppress uridine salvage in cells.
|
-
- HY-114996
-
|
|
Others
|
Inflammation/Immunology
|
|
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
|
-
- HY-151928
-
|
|
JNK
|
Neurological Disease
|
|
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.
|
-
- HY-149991
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-56 (compound 12126065) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC50 value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier.
|
-
- HY-149279
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-7 is a potent, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 53, 973, 1039 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-7 shows significant neuroprotective effects. JNK3 inhibitor-7 has the potential for the research of Alzheimer’s disease (AD).
|
-
- HY-152539
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-54 is a potent HIV-1 inhibitor. HIV-1 inhibitor-54 has anti-HIV activity in MT-4 cells against WT HIV-1 (strain IIIB) with an EC50 value of 0.032 μM. HIV-1 inhibitor-54 can be used for the research of virus infection.
|
-
- 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-149280
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD).
|
-
- HY-151972
-
|
|
Epigenetic Reader Domain
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
|
-
- HY-126200
-
-
- HY-103036
-
-
- HY-114311
-
|
|
FGFR
Discoidin Domain Receptor
|
Cancer
|
|
FGFR1/DDR2 inhibitor 1 is an orally active inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM and 3.2 nM, respectively. Antitumor activity.
|
-
- HY-139376
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer.
|
-
- HY-155054
-
|
|
Parasite
|
Infection
|
|
Cysteine protease inhibitor-3 (Compound 15) is a Cysteine protease inhibitor. Cysteine protease inhibitor-3 inhibits Pf3D7, PfW2, PfFP2 and PfFP3 with IC50s of 0.74 μM, 1.05 μM, 3.5 μM, and 4.9 μM, respectively. Cysteine protease inhibitor-3 has anti-plasmodial efficacy against both drug-sensitive and drug-resistant parasites.
|
-
- HY-N11906
-
|
Syringaresinol dimethyl ether; Lirioresinol C dimethyl ether
|
Others
|
Inflammation/Immunology
|
|
Diayangambin (Syringaresinol dimethyl ether; Lirioresinol C dimethyl ether) is a cell proliferation inhibitor with an IC50 value of 1.5 μM against human monocytes. Diayangambin also has immunosuppressive and anti-inflammatory effects.
|
-
- HY-150759
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-45 (compound IA-6) is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity.
|
-
- HY-146089
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-32 (compound 3c) is a potent HIV-1 inhibitor with an IC50 value of 34 nM for WT HIV-1. HIV-1 inhibitor-32 can be used for researching AIDS.
|
-
- HY-153017
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.
|
-
- HY-119369
-
|
|
Bacterial
|
Infection
|
|
FadD32 Inhibitor-1 is a potent FadD32 inhibitor with anti-tubercular activity.
|
-
- HY-P34013
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Urinary Trypsin Inhibitor Fragment is a fragment derived from urinary trypsin inhibitor by proteolysis. Urinary Trypsin Inhibitor Fragment can inhibit tumor cell invasion by limited proteolysis.
|
-
- HY-110077
-
|
|
Akt
Apoptosis
|
Cancer
|
|
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL).
|
-
- HY-156437
-
|
|
Ser/Thr Protease
Apoptosis
|
Cancer
|
|
NBI-961 is a potent NEK2 inhibitor that inhibits proteasomal degradation. NBI-961 induces G2/mitosis arrest and apoptosis in diffuse large B cell lymphoma (DLBCL) cells.
|
-
- HY-139077
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
Metabolic Disease
|
|
SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer.
|
-
- HY-117997
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor.
|
-
- HY-19763
-
|
PI3Kα Inhibitor 1
|
PI3K
|
Cancer
|
|
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
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- HY-12652
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mTOR
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Cancer
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AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K.
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- HY-148273
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PROTACs
Ras
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Cancer
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KRAS G12D inhibitor 17 (example 8) is a quinazoline-linked (4R)-4-hydroxy-L-prolinamide compound, inducing degradation of G12D-mutation KRAS protein. KRAS G12D inhibitor 17 is a PROTAC.
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- HY-139639
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MEK
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Cancer
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MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
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- HY-139638
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MEK
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Cancer
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MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
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- HY-153714
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BNM-1192; Menin-MLL Inhibitor 27
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Epigenetic Reader Domain
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Cancer
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Menin-MLL inhibitor 27 can inhibit the Menin-MLL interaction and can be used in cancer research, such as acute myeloid leukemia.
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- HY-10862
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Benzothiazole analog 3
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FAAH
Autophagy
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Cancer
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FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
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- HY-147370
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HIV
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Infection
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HIV-1 inhibitor-46 (compound 13d) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor with an EC50 value of 1.425 μM. HIV-1 inhibitor-46 can be used for the research of AIDS.
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- HY-155493
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Cytochrome P450
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Cancer
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CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and
aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer.
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- HY-119823
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P-glycoprotein
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Cancer
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PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin.
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- HY-112614
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ATM/ATR
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Cancer
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ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.
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- HY-147552
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HIV
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Infection
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HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent.
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- HY-147723
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HIV
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Infection
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HIV-1 inhibitor-39 (compound 3c) is a potent HIV-1 inhibitor with an EC50 of >112.88 µM. HIV-1 inhibitor-39 shows anti-RT (HIV-1 reverse transcriptase) activities with an IC50 of 15.75 µM. HIV-1 inhibitor-39 shows cytotoxicity for MT-4 cells with an CC50 of 112.9 µM.
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- HY-148042
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HIV
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Infection
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HIV-1 inhibitor-47 is an inhibitor of HIV-1, and inhibits vif-dependent degradation of human APOBEC3G, with an IC50 value of 14.33 μM. HIV-1 inhibitor-47 also involves in derivatives of 1-(2-pyrimidinyl)piperazine synthesis, with potential antianxiety, antidepressant, and antipsychotic effect.
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- HY-147903
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HIV
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Infection
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HIV-1 inhibitor-42 (compound 5b) is a potent HIV-1 inhibitor, with an IC50 of 0.06 μM. HIV-1 inhibitor-42 inhibits HIV-1 RT RNA-dependent DNA polymerase and DNA-dependent DNA polymerase, with IC50 values of 0.518 and 0.072 μM.
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- HY-155078
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer.
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- HY-121762
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Acyltransferase
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Cardiovascular Disease
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NTE-122 (dihydrochloride) is an inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with the IC50 in liver and aorta of cholesterol-fed rabbits of 7.6nM, 4.4nM and 9.6 nM, respectively, that plays an important role in atherosclerosis.
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- HY-128722
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HIV
|
Infection
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HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927.
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- HY-108255
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HIV
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Infection
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HIV-1 inhibitor-60 (compound 45) is an HIV inhibitor with the potential for the research of infection diseases.
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- HY-155648
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Bacterial
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Infection
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Tuberculosis inhibitor 6 (compound 2c) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of ≤1.66 μM) and Mycobacterium marinum (MIC90 of 2.65 μM).
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- HY-155649
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Bacterial
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Infection
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Tuberculosis inhibitor 7 (compound 2d) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of 0.63 μM) and Mycobacterium marinum (MIC90 of 0.63 μM).
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- HY-155651
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Bacterial
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Infection
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Tuberculosis inhibitor 9 (compound 3d) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of 0.64 μM) and Mycobacterium marinum (MIC90 of 0.64 μM).
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- HY-155650
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|
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Bacterial
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Infection
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Tuberculosis inhibitor 8 (compound 3b) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacterium tuberculosis (MIC90 of 0.69 μM) and Mycobacterium marinum (MIC90 of 0.69 μM).
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- HY-150697
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HIV
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Others
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HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM.
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- HY-112136
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CP 43
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MAP3K
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Cancer
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TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
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- HY-23338
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PARP
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Others
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TNKS-2-IN-1 (Compound 13g) is a TNKS-2 inhibitor. TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM.
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- HY-155344
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-38 (Compound 11j) is a potent inhibitor of α-glucosidase inhibitor with IC50 of 12.44±0.38 μM.α-Glucosidase-IN-38 plays an important role in Diabetes mellitus (DM).
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- HY-136279
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Apoptosis
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Cancer
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TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
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- HY-100211
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TAPI-2
4 Publications Verification
TNF Protease Inhibitor 2
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MMP
SARS-CoV
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Cancer
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TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
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- HY-153668A
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- HY-112843
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|
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Others
|
Others
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CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
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- HY-P3065
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Calcium Channel
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Neurological Disease
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Calcicludine is a protein toxin from the venom of the green mamba Dendroaspis angusticeps that inhibits high-voltage-activated calcium channel, especially L-type calcium channel with the IC50 of 88 nM. Calcicludine has role in excitatory synaptic transmission.
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- HY-157124
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