Search Result
Results for "
inhibit
" in MedChemExpress (MCE) Product Catalog:
9941
Inhibitors & Agonists
20
Biochemical Assay Reagents
90
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-157039
-
|
|
RIP kinase
|
Inflammation/Immunology
|
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RIPK1/3-IN-17 (Compound 10) is a RIPK1 and RIPK3 inhibitor. RIPK1/3-IN-17 specifically inhibits necroptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation .
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-
-
- HY-10250A
-
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TCN-P sodium
|
ATP Synthase
|
Metabolic Disease
Cancer
|
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Triciribine phosphate sodium inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate sodium also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity .
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-
-
- HY-162971
-
|
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Ras
|
Cancer
|
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KRAS inhibitor-33 (compound 115a) is an inhibitor of pyridopyrimidine kras (IC50 ≤ 100nM) .
|
-
-
- HY-162294
-
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c-Myc
|
Cancer
|
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c-Myc inhibitor 13 (compound A6) is a c-MYC transcription inhibitor. c-Myc inhibitor 13 selectively stabilizes c-MYC G4 and inhibits G4-associated c-MYC transcription .
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-
-
- HY-131005
-
-
-
- HY-160445
-
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Others
|
Cancer
|
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KRAS G12D inhibitor 19 (Compound 7) is a KRAS G12D inhibitor. KRAS G12D inhibitor 19 can be used for the research of cancer .
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-
-
- HY-N12405
-
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Calmodulin
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Others
|
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Encecalinol, extracted from aerial parts of Ageratina grandifolia, is a potent inhibitor of calmodulin inhibitor .
|
-
-
- HY-163173
-
|
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YAP
|
Cancer
|
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TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells .
|
-
-
- HY-W739700
-
|
d-Aminoglutethimide L-Tartrate
|
Cytochrome P450
|
Inflammation/Immunology
|
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(R)-(+)-Aminoglutethimide (L-Tartrate) is an inhibitor of aromatase. (R)-(+)-Aminoglutethimide inhibits androstenedione with a Ki value of 0.3 μM .
|
-
-
- HY-117194
-
|
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HIV
GSK-3
|
Infection
|
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18BIOder is a neuroprotective GSK-3β inhibitor, highly selectively inhibiting HIV-1 .
|
-
-
- HY-113753
-
|
|
Antibiotic
|
Infection
|
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PDF-IN-1 (compound 2) is a potential Peptide deformylase (PDF) inhibitor. PDF-IN-1 can be used for the development of new broad-spectrum antibiotics 。
|
-
-
- HY-10250
-
|
TCN-P
|
ATP Synthase
|
Metabolic Disease
Cancer
|
|
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-118525
-
|
|
HCV
PI4K
|
Infection
|
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AL-9 is a inhibitor of PI4KIIIα, with the IC50 of 0.57 μM, that can inhibit HCV replication .
|
-
-
- 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 .
|
-
-
- HY-157306
-
|
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URAT1
|
Metabolic Disease
|
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HC-1310 URAT1 Inhibitor (Compound 83) is a potent URAT1 inhibitor and can be used for research on hyperuricemia and gout .
|
-
-
- HY-134929
-
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Hexokinase
|
Infection
Cancer
|
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Hexokinase 2 inhibitor 1 (Compound 2a) is a hexokinase 2 (HK2) inhibitor with anti-tumor activity and can be used in cancer research .
|
-
-
- HY-14412
-
|
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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-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 .
|
-
-
- HY-162041
-
|
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Survivin
|
Cancer
|
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AQIM-I is an inhibitor of survivin via inhibits survivin expression and colony formation. AQIM-I induces ROS production, apoptosis, cell cycle arrest, DNA damage, and autophagy. AQIM-I inhibits nonsmall cell lung cancer cells A549 with an IC50 value of 9 nM .
|
-
-
- HY-157122
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VJDT
1 Publications Verification
|
Others
|
Cancer
|
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VJDT is a TREM1 small molecule inhibitor that effectively blocks TREM1 signaling. VJDT inhibits tumor growth and can be used in cancer research .
|
-
-
- HY-157322
-
|
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Others
|
Infection
|
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SAV13 is an inhibitor of SaeR. SAV13 is an analogue of HR3744. SAV13 inhibits SaeR-DNA probe binding and has antivirulence properties .
|
-
-
- HY-168006
-
|
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p97
ATP Synthase
|
Cancer
|
|
NSC819701 is a triazole inhibitor of the p97 ATPase. NSC819701 inhibits the activity of p97 ATPase by binding to a specific site of p97 .
|
-
-
- HY-162086
-
|
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HDAC
|
Cancer
|
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HDAC-IN-68 (Compound 29) is a potent HDAC inhibitor that disrupts microtubule structure and inhibits tumor growth. HDAC-IN-68 significantly inhibits class I HDACs (HDAC1, HDAC2, HDAC3) with IC50 values of 5.1, 11.5 and 8.8 nM, respectively .
|
-
-
- HY-156781
-
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Sirtuin
|
Metabolic Disease
|
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Sirtuin-1 inhibitor 1 (Compound 8) is an inhibitor of Sirtuin-1 that plays important roles in obesity-induced diabetes and aging-related diseases .
|
-
-
- HY-155482
-
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Others
|
Neurological Disease
|
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NA-184 is a selective calpain-2 inhibitor. NA-184 inhibits TBI-induced cell death with an EC50 of 0.13 mg/kg .
|
-
-
- HY-149718
-
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JAK
HDAC
|
Cancer
|
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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 .
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-
-
- HY-163088
-
|
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Flavivirus
|
Infection
|
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CHIKV-IN-4 (compound 31b) is a potent and selective CHIKV inhibitor. CHIKV-IN-4 inhibits the Chikungunya virus with the EC50 value of 0.6 μM .
|
-
-
- HY-157148
-
|
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c-Met/HGFR
Trk Receptor
|
Cancer
|
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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-162091
-
|
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Topoisomerase
|
Cancer
|
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Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo .
|
-
-
- HY-122874
-
-
-
- HY-149665
-
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DGK
|
Cancer
|
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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-34386
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
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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-155587
-
|
|
Others
|
Cancer
|
|
Hydroxy-PP is a potent CBR1 inhibitor with an IC50 value of 0.78 μM. Hydroxy-PP also potently inhibits the cytoplasmic tyrosine kinase Fyn with an IC50 value of 5 nM .
|
-
-
- 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) .
|
-
-
- HY-149004B
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
SLF1081851 (hydrochloride) is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 (hydrochloride) plays a key role in the development and immune system .
|
-
-
- HY-107622
-
|
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Others
|
Metabolic Disease
|
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(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 .
|
-
-
- HY-156373
-
|
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Others
|
Others
|
|
MN714 is a pivaloyloxymethyl (POM) protected inhibitor .
|
-
-
- HY-117124
-
-
-
- HY-160499
-
-
-
- HY-15323
-
|
P505-15 Hydrochloride
|
Syk
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
Src
|
Cancer
|
|
PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models .
|
-
-
- HY-W404002
-
|
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Prolyl Endopeptidase (PREP)
|
Metabolic Disease
|
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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
|
-
-
- HY-P5988
-
|
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PKC
|
Cancer
|
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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-121710
-
|
7-Monohydroxyethylrutoside
|
Others
|
Cardiovascular Disease
|
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MonoHER (7-Monohydroxyethylrutoside) is a Carbonyl reductase 1 (CBR1) inhibitor and can be used as a cardioprotective agent. MonoHER inhibits the activity of CBR1 V88 and CBR1 I88 in a concentration-dependent manner .
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-
-
- HY-15324
-
|
P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate
|
Syk
Src
Mixed Lineage Kinase
PAK
Pyk2
FAK
Apoptosis
|
Cancer
|
|
PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models . .
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-
-
- HY-168005
-
|
|
p97
ATP Synthase
|
Cancer
|
|
NSC799462 is a triazole inhibitor of p97 ATPase. NSC799462 inhibits p97 ATPase activity (IC50 = 15 nM) by binding to a specific site on p97 and causing local changes in the p97 structure .
|
-
-
- HY-P5793
-
-
-
- HY-B0494
-
|
Bufexamic acid
|
HDAC
Aminopeptidase
|
Inflammation/Immunology
Cancer
|
|
Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
|
-
-
- HY-119374
-
|
|
Epigenetic Reader Domain
|
Cancer
|
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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 .
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-
-
- HY-161843
-
|
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Necroptosis
RIP kinase
|
Inflammation/Immunology
|
|
Necroptosis-IN-4, a potent necroptosis inhibitor, is a RIP kinase 1 (RIPK1) inhibitor. Necroptosis-IN-4 has no inhibitory activity against RIPK3 and weak inhibitory activity against VEGFR1/2 and PDGFR-α .
|
-
-
- HY-148249
-
|
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MALT1
|
Cancer
|
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NVS-MALT1 is a MALT1 allosteric inhibitor .
|
-
- HY-P5995
-
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Elastase
|
Cancer
|
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MeOSuc-AAPA-CMK is a potent inhibitor of human neutrophil elastase .
|
-
- HY-116238
-
|
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ROCK
|
Others
|
|
ROCK-IN-D2 is a potent and selective ROCK inhibitor .
|
-
- HY-161288
-
|
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PARP
|
Cancer
|
|
UKTT15 (compound 6) is an allosteric inhibitor of PARP1 .
|
-
- 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-N3464
-
|
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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-126388
-
-
- HY-P5179
-
|
HWTX-I
|
Calcium Channel
Sodium 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-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-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-169106
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase inhibitor 4 (compound 45) is a potent Topoisomerase1/2 inhibitor. Topoisomerase inhibitor 4 causes cell cycle arrest in the G2/M phase by inducing Apoptosis. Topoisomerase inhibitor 4 has antitumor activity .
|
-
- HY-160107
-
-
- HY-114256
-
|
|
PSMA
|
Cancer
|
|
EC1169 is a specific PSMA ligand that inhibits the growth of PSMA-positive cells .
|
-
- 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-157403
-
|
|
SARS-CoV
|
Infection
|
|
Jun12682 is an inhibitor of SARS-CoV-2 papain-like protease. Jun12682 inhibits PL pro with a Ki value of 37.7 nM. Jun12682 has EC50 value of 1.1 μM in the FlipGFP PL pro assay. Jun12682 has orally activity .
|
-
- HY-157254
-
|
|
Glutaminase
|
Cancer
|
|
AA10 is a potent and irreversible transglutaminase 2 (TG2) inhibitor for cancer research .
|
-
- HY-W171611
-
-
- HY-B0494R
-
|
|
HDAC
Aminopeptidase
|
Inflammation/Immunology
Cancer
|
|
Bufexamac (Standard) is the analytical standard of Bufexamac. This product is intended for research and analytical applications. Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 μM and 0.22 μM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
|
-
- HY-121213
-
|
|
Cytochrome P450
|
Cancer
|
|
Erysolin is a CYP1A inhibitor with antigenic toxicity. Erysolin reduces benzo(a)pyrene-induced genotoxicity .
|
-
- HY-101214A
-
|
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PAI-1
|
Others
|
|
UK-371804 hydrochloride (compound 24) is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM .
|
-
- HY-164315
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 67 (example 35) is a KRAS G12C inhibitor that selectively inhibits the growth of many KRAS G12C mutant tumor cell lines .
|
-
- HY-146709
-
-
- 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-161686
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 24 (Compound 11) is a human carbonic anhydrase (carbonic anhydrase) inhibitor. Ki values of Carbonic anhydrase inhibitor 24 for hCAs IX and XII were 10.7 and 7.5 nM, respectively .
|
-
- HY-121086
-
-
- HY-159611
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 68 (compound I-063) is a KRAS G12C inhibitor with an IC50 of 7 nM. KRAS G12C inhibitor 68 has anti-tumor activity .
|
-
- HY-139589
-
|
ISC-27864; GRC-27864
|
PGE synthase
|
Neurological Disease
Inflammation/Immunology
|
|
Zaloglanstat (ISC-27864) is a selective and orally active inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 5 nM. Zaloglanstat inhibits PGE2 release of IC50 at 161 nM and 154 nM in whole blood of pigs and dogs, respectively. Zaloglanstat can be used in studies of asthma, osteoarthritis and neurodegenerative diseases .
|
-
- HY-118715
-
-
- HY-101294
-
-
- 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-161077
-
|
|
Amyloid-β
|
Cancer
|
|
QP5020 (compound 28) is an inhibitor of QPCTL with an IC 50 value of 15 nM. QP5020 has antitumor efficacy .
|
-
- HY-157450
-
|
|
Apoptosis
|
Cancer
|
|
YF-Mo1 (compound 9) is a CBR1 inhibitor with an IC50 value of 1.1 μM .
|
-
- HY-160670
-
-
- HY-160671
-
-
- HY-129298
-
|
|
Aminopeptidase
|
Others
|
|
Amastatin is A slow, tightly bound, competitive inhibitor of aminopeptidase (AP) with an IC50 of 0.54 μg/mL for AP-A .
|
-
- HY-157308
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 10 (compound a8) inhibits the activity of α-Syn aggregation with low IC50 value (1.08 μM). α-Synuclein inhibitor 10 exhibits good binding affinity to α-Syn residues. α-Synuclein inhibitor 10 can be used in the research of Parkinson's disease (PD) .
|
-
- HY-P10066
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL inhibitor 31 (compound 18) is a potent inhibitor of the menin MLL interaction with an IC50 value of 4.6 nM .
|
-
- HY-123800
-
|
VTP-34072
|
11β-HSD
|
Neurological Disease
|
|
BI 187004 (VTP-34072) is an 11β-hydroxysteroid dehydrogenase 1 inhibitor for use in diabetes research .
|
-
- HY-161078
-
|
|
Amyloid-β
|
Cancer
|
|
QP5038 (compound 28) is an inhibitor of QPCTL with an IC50 value of 3.8 nM. QP5038 has antitumor efficacy .
|
-
- HY-160217
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-41 (compound Z389) is an inhibitor of HPK1 with an IC50 value of 0.21 nM .
|
-
- HY-160109
-
|
|
Mucin
|
Cancer
|
|
Ac5GalNTGc is a analog of hexosamine. Ac5GalNTGc inhibits mucin-type O-linked glycosylation biosynthesis .
|
-
- HY-162283
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-18 (compound 8z) is an inhibitor of FGFR4 and can be used in cancer research .
|
-
- 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-145826
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112 .
|
-
- HY-N0491
-
|
(-)-Lupinidine sulfate
|
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-156795
-
|
|
CDK
|
Cancer
|
|
PROTAC CDK9/CycT1 Degrader-2 is a inhibitor of CDK9, with the IC50 of 45 nM .
|
-
- HY-119592
-
-
- HY-157229
-
|
|
EGFR
|
Others
|
|
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .
|
-
- HY-160037
-
-
- HY-19286
-
|
F 12511
|
Acyltransferase
|
Cancer
|
|
Eflucimibe (F 12511) is a new acyl-coenzyme A cholesterol O-acyltransferase (ACAT) inhibitor. Eflucimibe can be used in the research of atherosclerosis .
|
-
- HY-157553
-
|
|
FAK
|
Cancer
|
|
FAK-IN-19 (ligand3) is an inhibitor in a co-crystal structure with FAK. FAK-IN-19 has anticancer effects .
|
-
- HY-P10149
-
|
|
Caspase
|
Cancer
|
|
Ac-IEPD-CHO is a reversible granzyme B inhibitor with a Ki of 80 nM . Ac-IEPD-CHO is also a caspase-8 inhibitor .
|
-
- HY-123326
-
|
|
Myosin
|
Infection
|
|
KT5926 is a potent selective myosin light chain kinase inhibitor that inhibits viral primary and secondary transcription and genomic RNA synthesis .
|
-
- HY-161412
-
|
|
HDAC
|
Cancer
|
|
STR-V-53 is an HDAC inhibitor (IC50 in nM).STR-V-53 increases histone acetylation in tumor cells by inhibiting the activity of these enzymes, which in turn regulates gene expression.STR-V-53 inhibits tumor growth, and induces apoptosis .
|
-
- HY-160007
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DHX9-IN-3 (Compound 621) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research .
|
-
- HY-160008
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DHX9-IN-4 (Compound 609) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research .
|
-
- HY-160010
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DHX9-IN-6 (Compound 620) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research .
|
-
- HY-136489A
-
|
|
PARP
|
Cancer
|
|
KU-0058948 hydrochloride is a specific and potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 hydrochloride shows anticancer effects .
|
-
- HY-12059B
-
|
|
Akt
|
Cancer
|
|
AT7867 hydrochloride is a potent and orally active inhibitor of AKT and p70 S6 kinase. AT7867 hydrochloride has anticancer effect .
|
-
- HY-162270
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-24 (compound 3f) is an inhibitor of cyclin-dependent kinase 2 with an elevated binding energy value .
|
-
- HY-101776A
-
|
Desmethyl-SB2343 hydrochloride
|
PI3K
mTOR
|
Cancer
|
|
Desmethyl-VS-5584 hydrochloride is a dimethyl analog of VS-5584, a potent and selective mTOR/< with a pyridine[2,3-d]pyrimidine structure. b>PI3KDual inhibitor .
|
-
- HY-401485
-
|
|
Pyk2
FAK
|
Cancer
|
|
Pyk2-IN-2 (compound 13j) is an inhibitor of Pyk2 with an IC50 of FAK kinase of 0.608 μM .
|
-
- HY-156819
-
|
KRAS G12D inhibitor 18
|
Ras
|
Cancer
|
|
RMC-9805 (KRAS G12D inhibitor 18) is a KRAS G12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling to induce apoptosis in KRAS G12D mutant cancer cells .
|
-
- 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-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-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-P10147
-
|
|
Caspase
|
Cancer
|
|
Ac-LDESD-AMC is a caspase-2 inhibitor. Ac-LDESD-AMC has a peptide sequence of Leu-Asp-Glu-Ser-Asp .
|
-
- HY-136727
-
|
|
Caspase
|
Cancer
|
|
Ac-LEVD-CHO is a caspase-4 inhibitor. Ac-LEVD-CHO is a peptide with the sequence of Ac-Leu-Glu-Val-Asp-al .
|
-
- HY-157889
-
|
|
HDAC
|
Cancer
|
|
ZINC000028464438 is a selective HDAC11 inhibitor with an IC50 of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes .
|
-
- HY-161293
-
|
|
p38 MAPK
|
Cancer
|
|
p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor .
|
-
- HY-149491
-
|
|
TAM Receptor
HIF/HIF Prolyl-Hydroxylase
|
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-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 .
|
-
- HY-157320
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
|
-
- 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-149720
-
-
- HY-161086
-
|
|
Bacterial
|
Infection
|
|
Antibiofilm agent-4 (compound 4p) is a LasR inhibitor. Antibiofilm agent-4 shows the best antibiofilm and anti-QS properties .
|
-
- HY-161051
-
|
|
NAMPT
DNA Alkylator/Crosslinker
|
Cancer
|
|
Anticancer agent 177 (Compound 11b) is a NAMPT inhibitor and DNA alkylating agent. Anticancer agent 177 has antitumor activity in vitro and in vivo .
|
-
- HY-136829
-
|
|
Others
|
Others
|
|
BPH-675 is a large bisphosphonate inhibitor with long hydrophobic side chains and a potent and selective geranylgeranyl diphosphate synthase (GGPPS) inhibitor with an IC50 of 0.71 μM .
|
-
- 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-162031
-
|
|
JAK
|
Metabolic Disease
|
|
MMT3-72-M2 is an MMT3-72 metabolite. MMT3-72-M2 is a selective JAK1 inhibitor. MMT3-72-M2 inhibits JAK1, JAK2, TYK2, and JAK3 with IC50 values of 10.8 nM, 26.3 nM, 91.6 nM, 328.7 nM, respectlly .
|
-
- HY-147165A
-
|
|
YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 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-162512
-
|
|
CCR
HIV
|
Infection
|
|
CB-0821 is a high affinity CCR5 inhibitor with a Ki of 0.04 nM. CB-0821 binds efficiently to the hydrophobic pocket of the CCR5 protein, to inhibit the interactions between viral protein and CCR5, thereby inhibiting viral entry. CB-0821 has the potential for anti-HIV research .
|
-
- HY-W587701
-
|
|
Bacterial
Antibiotic
|
|
|
Methacycline is a tetracycline antibiotic that inhibits bacterial protein synthesis. Methacycline is a potent inhibitor of epithelial-to-mesenchymal transition (EMT). Methacycline blocks EMT in vitro and inhibits fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline is an antimicrobial agent with potential for use in pulmonary fibrosis research .
|
-
- HY-156040
-
|
|
Casein Kinase
|
Cancer
|
|
Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685) .
|
-
- HY-148909
-
|
IDEFP
|
Cannabinoid Receptor
FAAH
|
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-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-112749
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ME-344 is a mitochondrial inhibitor. ME-344 has significant biological antitumor activity in HER2-negative breast cancer .
|
-
- HY-160211
-
|
|
Hippo (MST)
|
Cancer
|
|
JA310 is a highly selective MST3 kinase inhibitor. JA310 has high cellular potency against MST3 with an EC50 value of 106 nM .
|
-
- HY-161021
-
|
|
Adenylate Cyclase
|
Others
|
|
AC2 selective-IN-1 (compound 14) is a? potent (IC50=4.45 μM), non-toxic, and selective mAC2 inhibitor .
|
-
- HY-116792
-
-
- 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-160549
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 14 (Compound 13A) is a c-Myc protein inhibitor. The IC50 value of HL60 inhibitor is <100 nM. c-Myc inhibitor 14 shows antitumor activity .
|
-
- HY-155235
-
|
|
Steroid Sulfatase
|
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-18297
-
-
- 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-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-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-160167
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-30 (compound cpd15) is an inhibitor of Bruton's Tyrosine Kinase (BTK) and mutant BTK with IC50 values of 6.72 and 6.11nM respectively .
|
-
- 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-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-161028
-
|
|
Carbonic Anhydrase
Bacterial
|
Infection
|
|
Antibacterial agent 167 (compound 13) is an inhibitor of pathogenic bacterial carbonic anhydrases. Antibacterial agent 167 inhibits the growth of N. gonorrhea strains at concentrations ranging from 16 to 64 µg/mL .
|
-
- HY-163492
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 ( IC50 ≤10nM). PARP7-IN-19 can be used in the research area of tumors .
|
-
- HY-156784
-
|
DHX9-IN-2
|
DNA/RNA Synthesis
|
Cancer
|
|
ATX968 (example 31) is an inhibitor of ATP-dependent RNA helicase A (DHX9), with the EC50 of 0.054 μM in circBRIP1. ATX968 has antitumor activity .
|
-
- 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-16009B
-
|
(+)-Phenserine L-Tartrate; ANVS401 L-Tartrate
|
Amyloid-β
|
Cancer
|
|
Buntanetap (L-Tartrate) is an orally administered small molecule inhibitor of several neurotoxic proteins. Buntanetap reduces amyloid precursor protein (APP) production by blocking its mRNA translation .
|
-
- HY-157408
-
|
|
Histone Demethylase
|
Others
|
|
KDM4D-IN-3 (compound 1) is a small-molecule epigenetic inhibitor target at KDM4D with an IC50 value of 4.8 μM .
|
-
- HY-161277
-
|
|
17β-HSD
|
Cancer
|
|
HSD17B13-IN-100 (compound 34) is an inhibitor of HSD17B13 and has IC50 with estradiol ＜0.1 μM .
|
-
- HY-161278
-
|
|
17β-HSD
|
Cancer
|
|
HSD17B13-IN-100 (compound 37) is an inhibitor of HSD17B13 and has IC50 with Estradiol ＜0.1 μM .
|
-
- HY-161012
-
|
|
Apoptosis
|
Cancer
|
|
RB-07-16 is a C6-PyraP-BP inhibitor of human geranylammate pyrophosphate synthase (hGGPPS). RB-07-16 has antitumor activity .
|
-
- HY-156883
-
|
|
Cytochrome P450
|
Others
|
|
Dasatinib analog-1 (compound 5826) inhibits CYP3A4 viability with a Ki value of 5.4 μM. Dasatinib analog-1 blocks the formation of glutathione adducts .
|
-
- HY-N10227
-
-
- 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-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-16031B
-
|
NSC710464 dihydrochloride
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).
|
-
- HY-160859
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 8 (Example 224) is a WRN helicase inhibitor with IC50 value of 48 nM. WRN inhibitor 8 can be used in cancer research .
|
-
- HY-162854
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
Diacylglycerol acyltransferase inhibitor-2 (Example 8) is an inhibitor of Diacylglycerol Acyl Transferase 2 (DGAT2) with an IC50 value of 3.7 nM .
|
-
- 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-155170
-
|
|
Others
|
Cancer
|
|
MTDH-SND1 blocker 1 (compound C26-A6) is an inhibitor of the MTDH-SND1 protein. MTDH-SND1 blocker 1 inhibits cancer metastasis .
|
-
- HY-110031
-
|
|
Apoptosis
Bcl-2 Family
|
Cancer
|
|
BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases .
|
-
- 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-90009D
-
-
- HY-P10162
-
|
|
Caspase
|
Cancer
|
|
Ac-DMQD-AMC is an inhibitor of caspase-3. Ac-DMQD-AMC is an aromatic amine using aminium-based coupling reagent HATU in the presence of 2,4,6-trimethylpyridine (TMP) .
|
-
- HY-162035
-
-
- HY-157982
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-28 (compound 6J) is a selective butyrylcholinesterase (BChE) inhibitor with an IC50 of 8 nM and a Ki of 12.16 nM. BChE-IN-28 shows the lower inhibition against AChE, MAO-A and MAO-B .
|
-
- HY-P5942
-
-
- HY-P5943
-
-
- HY-P4306
-
-
- HY-163720
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS G12C inhibitor 63 (K45) is a KRAS G12C inhibitor. KRAS G12C inhibitor 63 can induce Apoptosis. KRAS G12C inhibitor 63 has antitumor activity .
|
-
- 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-169266
-
|
|
Bcl-2 Family
Apoptosis
|
Metabolic Disease
|
|
BRD-K56819078 is a Bcl-2 inhibitor that significantly reduces senescent cell load and senescence-related genes in the kidney mRNA expression. BRD-K56819078 exerts anti-aging effects by inhibiting apoptosis .
|
-
- HY-149311
-
|
|
Others
|
Others
|
|
PPO-IN-2 is an inhibitor of protoporphyrinogen IX oxidase with an Ki of 16 nM .
|
-
- HY-158157
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research .
|
-
- 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-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-160435
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-14 is a potent and selective TNFα inhibitor with an IC50 value of 1.1 µM. TNF-α-IN-14 shows antiinflammatory properties (WO2001072735A2; compound 12) .
|
-
- HY-160842
-
|
|
c-Fms
|
Neurological Disease
|
|
CSF1R-IN-24 (Example 134) is an orally active CSF1R inhibitor. CSF1R-IN-24 significantly inhibits the survival of human ipSC-derived microglia (hiPSC-MG) .
|
-
- HY-163519
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 13 is an inhibitor of α-synuclein (α-Syn). α-Synuclein inhibitor 13 inhibits the aggregation of α-Syn proteins and is able to break down formed fibers. It is mainly used in Parkinson's disease research .
|
-
- HY-N3632
-
|
Coronarin D Me ether
|
NF-κB
COX
|
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-157311
-
|
|
Glucosidase
|
Cancer
|
|
α-Glucosidase-IN-45 (compound 11E) is an inhibitor of α-glucosidase. α-Glucosidase-IN-45 is a novel indol-fused pyrano[2,3-D]pyrimidine compound .
|
-
- HY-162099
-
|
|
EGFR
|
Cancer
|
|
VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC50 value of 24.6nM against HCC827 cells .
|
-
- HY-18660B
-
|
PER977 acetate
|
Factor Xa
|
Cardiovascular Disease
|
|
Ciraparantag (PER977) acetate is a thrombin and factor Xa inhibitor. Ciraparantag acetate is a broad-spectrum reversal agent for anticoagulants, including low molecular weight heparins, unfractionated heparins, and some direct oral anticoagulants, but not VKAs .
|
-
- HY-N12537
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/ PD-L1-in-38 is a PD-1/PD-L1 inhibitor, which can inhibit the proliferation of tumor cells, promote the secretion of INF-γ by CD8 + T cells, and inhibit the ability of PD-1/PD-L1 signal transduction. PD-1/PD-L1-IN-38 has antitumor activity .
|
-
- HY-105246
-
|
|
Beta-lactamase
HDAC
Apoptosis
|
Cancer
|
|
Pracinostat dihydrochloride is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat dihydrochloride also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM .
|
-
- 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-120208
-
-
- HY-156877
-
-
- HY-106749
-
-
- HY-162100
-
|
|
ULK
Autophagy
|
Cancer
|
|
MR-2088 is a selective ULK1/ULK2 inhibitor with pEC50 values of 8.3 and 8.7, respectively. MR-2088 selectively inhibits autophagy through ULK1/2 mediated inhibition .
|
-
- HY-153986
-
|
|
Others
|
Neurological Disease
|
|
AEP-IN-2 is an asparagine endopeptidase (AEP) inhibitor via block AEP cleavage of APP and Tau. AEP-IN-2 has oral activity and decreases Aβ40 and Aβ42 and p-Tau levels .
|
-
- HY-163133
-
|
|
PIKfyve
|
Cancer
|
|
PIKfyve-IN-3 (compound L22) has a remarkable interaction with PIKfyve kinase with a Kd value of 0.47 nM. PIKfyve-IN-3 has oral activity. PIKfyve-IN-3 inhibits tumor growth in a HeLa xenograft model .
|
-
- HY-158039
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors .
|
-
- HY-157391
-
-
- 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-136728
-
|
|
Caspase
|
Cancer
|
|
Ac-YVAD-AOM is the inhibitor of caspase-1 that shows antitumor activity .
|
-
- HY-134382
-
|
7-Deaza-2'-deoxyadenosine-5'-O-diphosphate
|
Others
|
Others
|
|
7-CH-dADP is a competitive inhibitor or regulator of enzymes that interact with dADP .
|
-
- HY-162903
-
|
|
Parasite
|
Infection
|
|
LN002 is an orally active anti-Cryptosporidium oxidase inhibitor for the study of cryptosporidiosis .
|
-
- HY-164358
-
-
- HY-169168
-
|
|
Others
|
Others
|
|
Herbicidal agent 6 (D15) is a Transketolase (TKL) inhibitor with herbicidal 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-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-118712
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor WYE-23 is a mTOR inhibitor, and IC50 is 0.45 nM. It is selective to PI3Kα and IC50 is 661 nM. mTOR inhibitor WYE-23 has antitumor activity .
|
-
- HY-161328
-
|
|
Monoamine Oxidase
α-synuclein
Tau Protein
|
Neurological Disease
|
|
MAO-B-IN-31 (Compound 30) is an effective and selective inhibitor of monoamine oxidase B (monoamine oxidase B). The IC50 value is 41 nM. MAO-B-IN-31 also inhibits α-syn and tau aggregation. MAO-B-IN-31 has neuroprotective activity .
|
-
- HY-164718
-
|
|
EGFR
|
Cancer
|
|
Sevabertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor activity .
|
-
- 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-156782
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DHX9-IN-1 (example 160) is an inhibitor of ATP-dependent RNA helicase A (DHX9), with an EC50 value of 6.94 μM in DHX9 cellular target engagement. DHX9-IN-1 has antitumor activity .
|
-
- 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-N12507
-
|
|
STING
NF-κB
|
Others
|
|
Eupenicisirenin C (compound 1) is a sirenin derivative. Eupenicisirenin C has strong NF-κB inhibitory activities. Eupenicisirenin C suppresses effects on cGAS-STING pathway. Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells .
|
-
- HY-112546
-
|
|
MMP
|
Cancer
|
|
MMP-2 Inhibitor I (OA-Hy) is a potent MMP-2 inhibitor with a Ki of 1.7 μM .
|
-
- HY-163787
-
|
|
CDK
|
Cancer
|
|
YY173 is a dual inhibitor for CDK4 and CDK6 with IC50 of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC50 of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786) .
|
-
- HY-12429A
-
|
BMS-791325 hydrochloride
|
HCV
|
Infection
|
|
Beclabuvir (BMS-791325) hydrochloride is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM .
|
-
- 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-152170
-
|
|
nAChR
|
Neurological Disease
|
|
bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
|
-
- HY-162078
-
|
|
Casein Kinase
|
Cancer
|
|
Antiproliferative agent-46 (compound 5e) is an inhibitor of the casein kinase-2 enzyme (CK2) receptor. Antiproliferative agent-46 has a potent antiproliferative activity with an IC50 value of 5.75 μM on the U87 cell line .
|
-
- HY-162275
-
|
|
Others
|
Cancer
|
|
JMJD1C-IN-1 (compound 193D7) is an inhibitor of JMJD1C with oral activity. JMJD1C-IN-1 targets tumor Treg cells without affecting systemic immune homeostasis .
|
-
- HY-P10072A
-
|
Hsp25 kinase inhibitor acetate; Mk2 pseudosubstrate acetate
|
JNK
HSP
MAPKAPK2 (MK2)
p38 MAPK
ERK
|
Others
|
|
MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-144708
-
|
|
TAM Receptor
|
Cancer
|
|
Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC50 of 28.8 μM .
|
-
- HY-P2949
-
|
|
Potassium Channel
|
Cancer
|
|
Pandinotoxin Kα, isolated from the venom of Pandinus imperator, is the inhibitor of A-type potassium channel .
|
-
- HY-123322
-
-
- HY-163576
-
|
|
Others
|
Cancer
|
|
GID4-IN-1 (compd 169) is a GID4 inhibitor with an IC50 <500 nM .
|
-
- HY-119025
-
-
- HY-122795
-
|
|
Thymidylate Synthase
|
Others
|
|
Vanoxonin is an inhibitor of thymidylate synthase found in Saccharopolyspora hirsuta with an IC50 value of 0.7 μg/mL .
|
-
- 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-169085
-
|
|
Others
|
Metabolic Disease
|
|
LRAT-IN-1 (compound 1) is a retinol acyltransferase (LRAT) inhibitor (IC50=21.1 μM). LRAT-IN-1 provides anti-aging effects by inhibiting the esterification of retinol to form retinol esters, increasing the available retinol in the skin. Research on LRAT-IN-1 as an anti-aging ingredient in cosmetics .
|
-
- 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-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-121935
-
|
|
Fungal
|
Infection
|
|
Tecnazene (2,3,5,6-Tetrachloronitrobenzene) is a fungicide and is used as a sprout inhibitor on stored potatoes .
|
-
- 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-P5938
-
|
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable caspase-1 inhibitor that has antitumor activity .
|
-
- HY-P5955
-
|
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity .
|
-
- HY-149699
-
