Search Result
Results for "An animation that enzyme Inhibitors" in MCE Product Catalog:
9293
Inhibitors & Agonists
32
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-124861
-
-
- HY-U00439
-
-
- HY-108285
-
|
(Rac)-Telmesteine
|
Others
|
Inflammation/Immunology
|
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(Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents.
|
-
- HY-116677
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- HY-W015495
-
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- HY-33914
-
-
- HY-B1368
-
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Fenclonine
4-Chloro-DL-phenylalAnine; PCPA; CP-10188
|
Tryptophan Hydroxylase
|
Others
|
|
Fenclonine is a potent and irreversible inhibitor of tryptophan (Trp) hydroxylase, the rate-limiting enzyme in serotonin biosynthesis.
|
-
- HY-125965
-
|
BioA-IN-13
|
Bacterial
|
Infection
|
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BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
|
-
- HY-107393
-
-
- HY-100527
-
|
AN2718
|
Fungal
|
Infection
|
|
AN2718 inhibits fungal growth by blocking protein synthesis using the oxaborole tRNA trapping (OBORT) mechanism.
|
-
- HY-18325
-
-
- HY-19830
-
-
- HY-B2192
-
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Amylase
|
Others
|
Metabolic Disease
|
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Amylase is an enzyme produced by pancreas and salivary glands, catalyzing the hydrolysis of starch into sugars. Amylase are broadly classified into α, β, and γ subtypes.
|
-
- HY-128337
-
|
AN7973
|
Parasite
|
Infection
|
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AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting drug candidate for treating cryptosporidiosis.
|
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- HY-128204
-
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AN3661
|
Parasite
|
Infection
|
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AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.
|
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- HY-B0384
-
-
- HY-118660
-
|
Anhydrotetracycline hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
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Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells.
|
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- HY-111543
-
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AN11251
|
Parasite
|
Infection
|
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AN11251 is a potent and oral active anti-Wolbachia agent with potential for treatment of onchocerciasis and lymphatic filariasis, with EC50 values of 1.5 nM in LDW1 cell lines and 15 nM in C6/36 cell lines.
|
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- HY-100296
-
-
- HY-115537
-
|
NAE-IN-M22
|
Apoptosis
|
Cancer
|
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NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-111558
-
|
Bobcat339
|
DNA Methyltransferase
|
Cancer
|
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Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
-
- HY-120508
-
|
Pivanex
An-9; Pivalyloxymethyl butyrate
|
HDAC
Bcr-Abl
Apoptosis
|
Cancer
Inflammation/Immunology
|
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Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.
|
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- HY-10978
-
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- HY-130569
-
|
7-Hydroxymethotrexate
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Drug Metabolite
|
Cancer
Inflammation/Immunology
|
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7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
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- HY-131005
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-
- HY-135470
-
|
Nifurpirinol
P-7138
|
Antibiotic
Bacterial
|
Infection
|
|
Nifurpirinol (P-7138) is a nitroaromatic antibiotic and acts as a novel substrate for the bacterial nitroreductase (NTR) enzyme. Nifurpirinol is a more potent prodrug compared to Metronidazole to trigger cell-ablation in nitroreductase expressing transgenic models.
|
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- HY-10980
-
|
Tavaborole
An-2690
|
Fungal
Antibiotic
|
Infection
|
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Tavaborole (AN-2690) is an antifungal agent with activity against Trichophyton species, in a topical solution formulation for the potential treatment of onychomycosis.
|
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- HY-U00040
-
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- HY-78961
-
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- HY-W030319
-
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- HY-19676
-
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Pralnacasan
VX-740; HMR 3480
|
Caspase
|
Inflammation/Immunology
|
|
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
|
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- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
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Protein kinase inhibitors 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.
|
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- HY-121879
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- HY-19910
-
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Acoziborole
SCYX-7158; An5568
|
Parasite
|
Infection
|
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Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL.
|
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- HY-130760
-
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- HY-19373
-
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- HY-108263B
-
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(R)-3-Hydroxy Midostaurin
(R)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
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(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
|
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- HY-135849
-
|
Catalase
|
Reactive Oxygen Species
|
Cancer
|
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Catalase is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger.
|
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- HY-130259
-
|
LC3-mHTT-IN-AN2
|
Autophagy
|
Neurological Disease
|
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LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
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- HY-130258
-
|
LC3-mHTT-IN-AN1
|
Autophagy
|
Neurological Disease
|
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LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
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- HY-108263A
-
|
(S)-3-Hydroxy Midostaurin
(S)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
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(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML).
|
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- HY-W012037
-
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8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
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8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
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- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
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Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
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- HY-115292
-
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Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
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- HY-113951
-
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- HY-P1044
-
|
Spinorphin
LVV-hemorphin-4
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Others
|
Neurological Disease
|
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Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
|
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- HY-U00459A
-
-
- HY-18643
-
|
TZ9
|
E1/E2/E3 Enzyme
|
Cancer
|
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TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
|
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- HY-10827
-
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- HY-135813
-
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LtaS-IN-1
|
Bacterial
|
Infection
|
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LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
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- HY-N2021A
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- HY-101918
-
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DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
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- HY-112205
-
-
- HY-101681
-
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- HY-B0263
-
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- HY-16787
-
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ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
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- HY-103112A
-
|
SB 243213 dihydrochloride
|
5-HT Receptor
|
Neurological Disease
|
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SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
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- HY-103112B
-
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SB 243213
|
5-HT Receptor
|
Neurological Disease
|
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SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
|
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- HY-103112
-
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SB 243213 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
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SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
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- HY-U00459
-
|
GSK2850163
|
IRE1
|
Cancer
|
|
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-109040
-
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Quilseconazole
VT-1129
|
Fungal
Cytochrome P450
|
Infection
|
|
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
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- HY-U00459B
-
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GSK2850163 hydrochloride
|
IRE1
|
Cancer
|
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GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
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- HY-18728
-
-
- HY-108321
-
-
- HY-B0331
-
-
- HY-U00041
-
-
- HY-125957
-
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A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-114304
-
|
COH000
|
E1/E2/E3 Enzyme
|
Cancer
|
|
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
|
-
- HY-B0242
-
-
- HY-B0655
-
-
- HY-B0607
-
-
- HY-16450
-
-
- HY-16560
-
-
- HY-P0143
-
-
- HY-B0279
-
-
- HY-U00074
-
-
- HY-107337
-
-
- HY-107994
-
-
- HY-112860
-
-
- HY-A0116S
-
-
- HY-W010538
-
-
- HY-B0093
-
-
- HY-B1202
-
|
Alrestatin
AY-22284
|
Aldose Reductase
|
Endocrinology
|
|
Alrestatin is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.
|
-
- HY-100312
-
-
- HY-B1451
-
-
- HY-B1202A
-
-
- HY-B0331A
-
-
- HY-A0043A
-
-
- HY-B0093A
-
-
- HY-A0043
-
-
- HY-13989
-
-
- HY-100615
-
-
- HY-18690A
-
-
- HY-15583
-
-
- HY-18081
-
|
PF 750
|
FAAH
Autophagy
|
Metabolic Disease
|
|
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile.
|
-
- HY-B0919
-
-
- HY-106446
-
-
- HY-16273A
-
-
- HY-B0231
-
-
- HY-B0477
-
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-124960
-
-
- HY-110079
-
|
TNP
|
Others
|
Cancer
|
|
TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC50 values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes.
|
-
- HY-B0882
-
|
Edrophonium chloride
|
AChE
|
Neurological Disease
|
|
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-N7060
-
-
- HY-114507
-
|
Flumioxazin
Sumisoya; V-53482
|
Others
|
Others
|
|
Flumioxazin (Sumisoya) is an herbicide for use in soybean and peanut. Flumioxazin inhibits the enzyme protoporphyrinogen oxidase.
|
-
- HY-111458
-
-
- HY-112861
-
-
- HY-119689
-
|
Umibecestat
CNP520
|
Beta-secretase
|
Neurological Disease
|
|
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively.
|
-
- HY-W010378
-
|
D-Asparagine
H-D-Asn-OH
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Asparagine (H-D-Asn-OH) is a competitive inhibitor of L-Asparagine hydrolysis with a Ki value of 0.24 mM. D-Asparagine is a source of nitrogen for yeast strains. D-Asparagine is a good substrate for the external yeast asparaginase but is a poor substrate for the internal enzyme.
|
-
- HY-N6714
-
|
Alternariol
|
Topoisomerase
|
Cancer
Infection
|
|
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties.
|
-
- HY-N7263
-
|
Galanthamine N-Oxide
|
AChE
|
Neurological Disease
|
|
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes.
|
-
- HY-125776
-
|
Kresoxim-methyl
BAS 490 F
|
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Kresoxim-methyl (BAS 490 F), a Strobilurin-based fungicide, inhibits the respiration at the complex III (cytochrome bc1 complex). Kresoxim-methyl binds to complex III from yeast with an apparent Kd of 0.07 μM proving a high affinity for this enzyme.
|
-
- HY-136614
-
|
H-Val-βNA
L-Valine β-naphthylamide
|
Others
|
Others
|
|
H-Val-βNA (L-Valine β-naphthylamide) can be used as an aminopeptidase and a Valine arylamidase substrate.
|
-
- HY-B0382
-
-
- HY-B0331AS
-
-
- HY-109059
-
-
- HY-16437
-
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-131312
-
|
Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
|
-
- HY-107373
-
|
β-Chloro-L-alanine
L-β-ChloroalAnine
|
Bacterial
|
Infection
|
|
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
|
-
- HY-B1093
-
|
Fenchlorphos
|
Parasite
AChE
|
Infection
|
|
Fenchlorphos, an organophosphate, is an insecticide. Fenchlorphos is an inhibitor of the enzyme acetylcholinesterase (AChE). Fenchlorphos is able to cause mitochondrial dysfunction.
|
-
- HY-B0027
-
-
- HY-18206
-
-
- HY-13344
-
-
- HY-N0125
-
-
- HY-111532
-
|
(3R,4R)-A2-32-01
|
Bacterial
|
Infection
|
|
(3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
|
-
- HY-76316
-
|
Bergaptol
5-Hydroxypsoralen; 4-Hydroxybergapten
|
Cytochrome P450
|
Cancer
|
|
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
|
-
- HY-B0744
-
|
Eflornithine
DFMO; MDL71782; RMI71782; α-difluoromethylornithine
|
Others
|
Infection
|
|
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-U00197
-
|
Tilmacoxib
JTE522; JTP19605; RWJ57504
|
COX
|
Inflammation/Immunology
|
|
Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
|
-
- HY-128586A
-
-
- HY-B0744A
-
|
Eflornithine hydrochloride
DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride
|
Others
|
Infection
|
|
Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-18062
-
|
Pyrimethamine
PirimecidAn; Pirimetamin; RP 4753
|
Antifolate
Parasite
|
Infection
|
|
Pyrimethamine(RP4753) is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).
|
-
- HY-128586
-
-
- HY-122591
-
-
- HY-N0356
-
|
(-)-Catechin gallate
(-)-Catechin 3-gallate; (-)-Catechin 3-O-gallate
|
COX
|
Cancer
|
|
(-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
|
-
- HY-U00171
-
|
SQ28603
SQ28,603; Squibb 28603
|
Neprilysin
|
Metabolic Disease
|
|
SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
|
-
- HY-B0378A
-
-
- HY-18206A
-
-
- HY-10825
-
-
- HY-B0231BS
-
-
- HY-101790A
-
-
- HY-10484
-
-
- HY-125826
-
|
Heptasaccharide Glc4Xyl3
|
|
Metabolic Disease
|
|
Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature.
|
-
- HY-114161
-
-
- HY-136211
-
-
- HY-18030
-
|
CEP-28122
|
ALK
|
Cancer
|
|
CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
|
-
- HY-70062
-
-
- HY-W003445
-
|
4-Bromo-3-hydroxybenzoic acid
|
Endogenous Metabolite
|
Neurological Disease
|
|
4-Bromo-3-hydroxybenzoic acid is a metabolite of Brocresine and a histidine decarboxylase (HDC) inhibitor with IC50s of 1 mM for both rat fetal and rat gastric HDC. 4-Bromo-3-hydroxybenzoic acid also inhibits aromatic-L-amino acid decarboxylase from hog kidney and rat gastric mucosa in vitro with IC50s of 1 mM for both enzymes.
|
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-117580
-
-
- HY-19762
-
-
- HY-B0744B
-
|
Eflornithine hydrochloride hydrate
DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate
|
Others
|
Cancer
|
|
Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-W020215
-
-
- HY-109592
-
-
- HY-B0231AS
-
-
- HY-114161A
-
-
- HY-N2165
-
-
- HY-N4090
-
-
- HY-15345
-
|
Tetrahydrouridine dihydrate
THU dihydrate; NSC-112907 dihydrate
|
Others
|
Cancer
|
|
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
|
-
- HY-112179
-
|
GSK180
|
Others
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition.
|
-
- HY-116872
-
|
MAC13772
|
Bacterial
|
Infection
|
|
MAC13772 is a potent inhibitor of the enzyme BioA (IC50=250 nM), the antepenultimate step in biotin biosynthesis. MAC13772 is a novel antibacterial compound.
|
-
- HY-112305
-
|
AZ32
|
ATM/ATR
|
Cancer
|
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-106887
-
|
SCH 32615
|
Others
|
Neurological Disease
|
|
SCH 32615 is an enkephalinase (the enzymes responsible for the degradation of endogenous enkephalins) inhibitor. SCH 32615 can enhance surgery- and pregnancy-induced analgesia in mice.
|
-
- HY-111421
-
-
- HY-13296
-
|
PYR-41
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
- HY-129056
-
|
Melagatran
|
Thrombin
|
Cardiovascular Disease
|
|
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion.
|
-
- HY-100640
-
-
- HY-N6739
-
-
- HY-13283
-
-
- HY-W028047
-
-
- HY-100365
-
|
Remetinostat
SHP-141
|
HDAC
|
Cancer
|
|
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-50737
-
|
DUB-IN-3
|
Deubiquitinase
|
Cancer
|
|
DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor extracted from reference compound 22c with an IC50 of 0.56 μM for USP8.
|
-
- HY-112862
-
|
Arg-AMS
|
Aminoacyl-tRNA Synthetase
|
Others
|
|
Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
|
-
- HY-12988
-
|
C527
|
Deubiquitinase
|
Cancer
|
|
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
|
-
- HY-B0873
-
|
Uniconazole
|
Cytochrome P450
|
Others
|
|
Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki=68 nM), a family of enzymes that catabolize Abscisic acid, and thus, suppress gibberellin and sterol biosynthesis.
|
-
- HY-112734
-
-
- HY-N6702
-
-
- HY-127146
-
|
Platensimycin
|
Antibiotic
Bacterial
|
|
|
Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
|
-
- HY-13438
-
|
AZD3839 free base
|
Beta-secretase
|
Cancer
|
|
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
|
-
- HY-18054
-
|
BVT 2733
|
Others
|
Inflammation/Immunology
|
|
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.
|
-
- HY-N2071
-
|
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
|
-
- HY-101255
-
|
ODQ
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
|
-
- HY-125999
-
|
EPI-589
|
Others
|
Neurological Disease
|
|
EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor. EPI-589 has the potential for the treatment of amyotrophic lateral sclerosis (ALS).
|
-
- HY-16677A
-
-
- HY-N0529
-
-
- HY-16752
-
|
Relebactam
MK-7655
|
Bacterial
|
Infection
|
|
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.
|
-
- HY-B1189
-
-
- HY-13635A
-
|
Finasteride acetate
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-13635
-
|
Finasteride
MK-906
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-B2220
-
|
Cellulase
|
Others
|
Others
|
|
Cellulase is an enzyme catalyzing the hydrolysis of certain linkages in cellulose and other carbohydrates.
|
-
- HY-15301
-
|
CC0651
|
E1/E2/E3 Enzyme
|
Cancer
|
|
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27 Kip1, as confirmed by dose-response analysis.
|
-
- HY-133624
-
|
1,1,3-Tribromoacetone
|
Others
|
Cancer
|
|
1,1,3-Tribromoacetone is an impurity of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- HY-112435
-
|
UCT943
|
PI4K
|
Infection
|
|
UCT943 is a next-generation Plasmodium falciparum PI4K inhibitor. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with an IC50 of 23 nM.
|
-
- HY-124781
-
|
ML406
|
Bacterial
Antibiotic
|
Infection
|
|
ML406 is a small molecule probe that shows anti-tubercular activity via M.tuberculosis BioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM. M.tuberculosis BioA is an enzyme involved in biotin biosynthesis in M.tuberculosis.
|
-
- HY-13560
-
|
AVN-944
VX-944
|
Others
|
Cancer
|
|
AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.
|
-
- HY-18169
-
|
MUT056399
Fab-001
|
Bacterial
|
Infection
|
|
MUT056399 (Fab-001) is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively.
|
-
- HY-W012595A
-
|
trans-Benzylideneacetone
trAns-Benzalacetone
|
Phospholipase
|
Inflammation/Immunology
|
|
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). trans-Benzylideneacetone is an immunosuppressant.
|
-
- HY-10237
-
|
Boceprevir
EBP 520; SCH 503034
|
HCV Protease
HCV
|
Infection
|
|
Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay.
|
-
- HY-15100
-
|
Balicatib
AAE581
|
Cathepsin
|
Inflammation/Immunology
|
|
Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
|
-
- HY-131009
-
|
Fluorescein-NAD+
|
PARP
|
Others
|
|
Fluorescein-NAD+ is an alternative to radiolabeled NAD and a substrate for ADP-ribosylation. Fluorescein-NAD+ can be used in PARP assays by fluorescence microscopy. Extinction Coefficient: 262 nm.
|
-
- HY-A0166A
-
|
Cilastatin sodium
MK0791 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct.
|
-
- HY-A0166
-
|
Cilastatin
MK0791
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct.
|
-
- HY-112157
-
-
- HY-13592
-
|
HDAC-IN-7
Chidamide impurity
|
HDAC
|
Cancer
|
|
HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
|
-
- HY-12493A
-
-
- HY-100283
-
-
- HY-12493B
-
-
- HY-B0511
-
-
- HY-P1068
-
|
Lysozyme
Muramidase
|
Bacterial
|
Infection
|
|
Lysozyme is an antimicrobial enzyme produced by animals that forms part of the innate immune system.
|
-
- HY-N0680
-
-
- HY-16594
-
|
Lactacystin
|
Proteasome
|
Neurological Disease
|
|
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
|
-
- HY-B2158
-
-
- HY-114424A
-
-
- HY-114424
-
-
- HY-10493
-
|
Cobicistat
GS-9350
|
Cytochrome P450
HIV
|
Infection
|
|
Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
|
-
- HY-12853
-
|
Mesotrione
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant.
|
-
- HY-B1876
-
|
Nicosulfuron
|
Others
|
Others
|
|
Nicosulfuron is a selective herbicide belonging to the sulfonylurea family. Nicosulfuron is commonly used as a post-emergence herbicide to protect maize crops from weeds. Nicosulfuron inhibits acetolactate synthase (ALS) enzyme activity.
|
-
- HY-129035
-
-
- HY-10865
-
|
LY2183240
|
FAAH
Autophagy
|
Neurological Disease
|
|
LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
|
-
- HY-W006230
-
|
Anthraflavic acid
|
Others
|
Cancer
|
|
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
|
-
- HY-F0003
-
-
- HY-B2118
-
-
- HY-N2464
-
-
- HY-W015007
-
|
Metyrosine
|
COX
|
Cardiovascular Disease
|
|
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.
|
-
- HY-N1255
-
|
Scoulerine
(-)-Scoulerine; Discretamine
|
Microtubule/Tubulin
Beta-secretase
Apoptosis
|
Cancer
|
|
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
|
-
- HY-B0592S
-
-
- HY-17543
-
|
ML-323
|
Deubiquitinase
|
Cancer
|
|
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
|
-
- HY-12493
-
-
- HY-100079
-
|
9-Propenyladenine
Mutagenic Impurity of Tenofovir Disoproxil; Tenofovir Impurity 2
|
HIV
|
Infection
|
|
9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
|
-
- HY-18690
-
-
- HY-112942A
-
|
CMP-Sialic acid sodium salt
CMP-Neu5Ac sodium salt
|
Others
|
Metabolic Disease
|
|
CMP-Sialic acid sodium salt (CMP-Neu5Ac sodium salt) is an allosteric inhibitor of UDP-GlcNAc 2-epimerase, the enzyme that initiates sialic acid synthesis. CMP-Sialic acid sodium salt provides a substrate for Golgi sialyltransferases.
|
-
- HY-16106
-
|
Talazoparib
BMN-673; LT-673
|
PARP
|
Cancer
|
|
Talazoparib (BMN-673) is a highly potent, orally available PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 and 0.87 nM, respectively. Talazoparib has antitumor activity.
|
-
- HY-N0579
-
|
Fraxin
Fraxoside
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fraxin isolated from Acer tegmentosum, F. ornus or A. hippocastanum, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action, anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme.
|
-
- HY-N2472
-
|
Medicagenic acid
CastAnogenin
|
Bacterial
|
Infection
|
|
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra L, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes. Medicagenic acid (Castanogenin) has low enzyme inhibitory activities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE.
|
-
- HY-109000
-
|
Afabicin
Debio 1450; AFN-1720
|
Bacterial
|
Infection
|
|
Afabicin (Debio 1450) is the prodrug of Debio1452, specifically targeting staphylococci without significant activity against other Gram-positive or Gram-negative species. Debio1452 is an inhibitor FabI, an enzyme critical to fatty acid biosynthesis in staphylococci.
|
-
- HY-131703
-
|
UGT8-IN-1
|
Others
|
Metabolic Disease
|
|
UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders.
|
-
- HY-15272
-
|
WAY-600
|
mTOR
|
Cancer
Inflammation/Immunology
|
|
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
|
-
- HY-B0150
-
|
Nicotinamide
Niacinamide; Nicotinic acid amide
|
Endogenous Metabolite
Sirtuin
|
Neurological Disease
Cancer
|
|
Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
|
-
- HY-P0318
-
-
- HY-119974
-
|
Caracemide
NSC-253272
|
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
|
Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide is a novel anticancer agent derived from a hydroxamic acid and has demonstrated to produce severe central nervous system (CNS) toxicity.
|
-
- HY-17567A
-
|
Heparin sodium salt
Sodium heparin; Sodium heparinate
|
Autophagy
|
Cardiovascular Disease
|
|
Heparin sodium salt (Sodium heparin) is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa. Heparin sodium salt significantly inhibits exosome-cell interactions.
|
-
- HY-70013
-
|
Abiraterone
CB-7598
|
Cytochrome P450
|
Cancer
|
|
Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
|
-
- HY-12219A
-
|
MSI-1436 lactate
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-12219
-
|
MSI-1436
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-14768
-
|
Favipiravir
T-705
|
DNA/RNA Synthesis
Influenza Virus
SARS-CoV
|
Infection
|
|
Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
|
-
- HY-14519
-
|
Methotrexate
Amethopterin; CL14377; WR19039
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- HY-W011094
-
|
Win 18446
|
Aldehyde Dehydrogenase (ALDH)
|
Endocrinology
|
|
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.
|
-
- HY-129554
-
|
cis-9,10-Epoxystearic acid
cis-9,10-EpoxyoctadecAnoic acid
|
Endogenous Metabolite
|
Others
|
|
cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) is an endogenous constituent in human blood and urine. cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) can be produced from oleic acid by enzymic and non-enzymic epoxidation.
|
-
- HY-10439
-
|
HPGDS inhibitor 1
|
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-13297
-
|
PYZD-4409
|
E1/E2/E3 Enzyme
|
Cancer
|
|
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
|
-
- HY-101930
-
|
BMS-816336
|
Others
|
Metabolic Disease
|
|
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
|
-
- HY-100079A
-
|
(Z)-9-Propenyladenine
(Z)-Mutagenic Impurity of Tenofovir Disoproxil
|
HIV
|
Infection
|
|
(Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
|
-
- HY-P1488
-
-
- HY-N0913A
-
|
Isomaltotriose
|
Others
|
Others
|
|
Isomaltotriose is a sugar from enzymic hydrolyzates of the dextran from Leuconostoc mesenteroides NRRL B-512.
|
-
- HY-B2237
-
-
- HY-B1320
-
|
Meclofenamate sodium
Meclofenamic acid sodium
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic acid sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-B0182
-
|
Carmofur
HCFU
|
Nucleoside Antimetabolite/Analog
SARS-CoV
Virus Protease
|
Cancer
|
|
Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC50 of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC50 of 24.3 μM.
|
-
- HY-100450
-
-
- HY-14519A
-
|
Methotrexate disodium
Amethopterin disodium; CL14377 disodium; WR19039 disodium
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- HY-19958
-
|
XEN907
|
Sodium Channel
|
Neurological Disease
|
|
XEN907 is a potent and spirooxindole blocker of NaV1.7, with an IC50 of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain.
|
-
- HY-B0476
-
|
Phenacetin
Acetophenetidin
|
COX
|
Inflammation/Immunology
|
|
Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats.
|
-
- HY-114175
-
-
- HY-101577
-
-
- HY-130241
-
|
Reverse transcriptase-IN-1
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme.
|
-
- HY-111383
-
-
- HY-W015332
-
|
Captopril EP Impurity D
3-Bromoisobutyric acid
|
Others
|
Others
|
|
Captopril EP Impurity D is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-137768
-
|
Captopril EP Impurity B
|
Others
|
Others
|
|
Captopril EP Impurity B is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-W013886
-
|
Captopril EP Impurity J
S-Acetylcaptopril
|
Others
|
Others
|
|
Captopril EP Impurity J is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-B0336
-
|
Pranoprofen
|
COX
Apoptosis
PGE synthase
|
Cancer
Inflammation/Immunology
|
|
Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.
|
-
- HY-137769
-
|
Captopril EP Impurity C
3-Mercaptoisobutyric acid
|
Others
|
Others
|
|
Captopril EP Impurity C is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-B0592
-
|
Trandolapril
RU44570
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Trandolapril (RU44570) is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI).
|
-
- HY-19614
-
|
BMS-795311
|
CETP
|
Cardiovascular Disease
|
|
BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively.
|
-
- HY-134728
-
|
LpxC-IN-7
|
Bacterial
|
Infection
|
|
LpxC-IN-7 is a LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with antibacterial activities. LpxC is a key enzyme for catalyzing and synthesizing the main component lipid A of outer membrane lipopolysaccharide of Gram-negative bacteria.
|
-
- HY-100877
-
-
- HY-137772
-
|
Captopril EP Impurity E
|
Others
|
Others
|
|
Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
|
-
- HY-N1407
-
-
- HY-118517
-
|
α-Hydroxytamoxifen
(E)-α-Hydroxy tamoxifen; α-OHTAM
|
Others
|
Cancer
|
|
α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
|
-
- HY-112688
-
|
H-Arg-4MβNA
|
Others
|
Others
|
|
H-Arg-4MβNA is a substrate for cathepsin H, used for the detection of enzyme activity in gel electrophoresis.
|
-
- HY-N6706
-
|
Enniatin complex
|
Bacterial
Acyltransferase
Apoptosis
|
Cancer
Infection
|
|
Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .
|
-
- HY-19414
-
-
- HY-108966
-
|
Kushenol C
|
Beta-secretase
|
Inflammation/Immunology
|
|
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.
|
-
- HY-119402
-
|
BCL6-IN-8c
|
Bcl-2 Family
|
Cancer
|
|
BCL6-IN-8c is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
|
-
- HY-B0876
-
|
Fomepizole
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.
|
-
- HY-100211
-
|
TAPI-2
TNF Protease Inhibitor 2
|
MMP
SARS-CoV
|
Cancer
|
|
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.
|
-
- HY-133116S
-
|
4-Hydroxyatomoxetine D3
|
Others
|
Neurological Disease
|
|
4-Hydroxyatomoxetine D3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor.
|
-
- HY-101494
-
|
LY3214996
|
ERK
|
Cancer
|
|
LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.
|
-
- HY-N6667
-
|
Glucovanillin
|
Others
|
Others
|
|
Glucovanillin extracted from green pods and simultaneously transformed to vanillin by a combination of enzyme activities involving cell wall degradation and glucovanillin hydrolysis.
|
-
- HY-Y0801
-
-
- HY-124909
-
|
(6R)-FR054
|
Apoptosis
|
Cancer
|
|
(6R)-FR054 is an active isomer of FR054. FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect. FR054induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptosis.
|
-
- HY-130794
-
|
ALK/ROS1-IN-1
|
ALK
ROS
|
Cancer
|
|
ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
|
-
- HY-N7514
-
|
Strictosidinic acid
|
5-HT Receptor
|
Neurological Disease
|
|
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice.
|
-
- HY-U00287
-
|
BACE-IN-1
|
Beta-secretase
|
Neurological Disease
|
|
BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
|
-
- HY-101451
-
|
PBIT
|
Histone Demethylase
|
Cancer
|
|
PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
|
-
- HY-A0230A
-
|
Spirapril hydrochloride
SCH 33844 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- HY-117275
-
|
Meclofenamic acid
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic Acid, a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker.
|
-
- HY-12812
-
|
Autotaxin modulator 1
|
Phosphodiesterase (PDE)
|
Cancer
Neurological Disease
|
|
Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer.
|
-
- HY-B1856
-
|
Haloxyfop
|
Others
|
Metabolic Disease
|
|
Haloxyfop is an aryloxyphenoxypropionic acid herbicide and is widely used in grass weeds in broad-leaf crops. Haloxyfop inhibits the acetyl coenzyme A carboxylase (EC 6.4.1.2) from corn seedling chloroplasts with an IC50 of 0.5 μM, but has no effect on this enzyme in pea.
|
-
- HY-B0760
-
|
Fenofibric acid
FNF acid
|
PPAR
COX
|
Metabolic Disease
|
|
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
|
-
- HY-119307
-
|
Apratastat
|
MMP
TNF Receptor
|
Cancer
|
|
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
|
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-17514
-
|
Itraconazole
R51211
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
|
-
- HY-P1244
-
-
- HY-107383
-
-
- HY-B0580A
-
-
- HY-13026
-
|
Idelalisib
CAL-101; GS-1101
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
|
-
- HY-107339
-
|
Deserpidine
Harmonyl
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
Neurological Disease
|
|
Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.
|
-
- HY-18733
-
-
- HY-N2571
-
|
Corydine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine.
|
-
- HY-136072
-
|
QPX7728-OH disodium
|
Bacterial
|
Infection
|
|
QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
|
-
- HY-N2533
-
-
- HY-15463
-
|
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-108474
-
|
Nolatrexed dihydrochloride
AG 337; Thymitaq
|
Thymidylate Synthase
|
Cancer
|
|
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity.
|
-
- HY-B0124A
-
|
Zonisamide sodium
AD 810 sodium; CI 912 sodium
|
Carbonic Anhydrase
Calcium Channel
Sodium Channel
|
Neurological Disease
|
|
Zonisamide sodium (AD 810 sodium) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide sodium has antiepileptic activity. Zonisamide sodium can be used for the rsearch for epilepsy, seizures and Parkinson's disease.
|
-
- HY-109015S
-
|
Tucidinostat D4
Chidamide D4; HBI-8000 D4; CS 055 D4
|
HDAC
|
Cancer
|
|
Tucidinostat D4 (Chidamide D4) is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively.
|
-
- HY-130515
-
|
Cdc7-IN-3
|
CDK
|
Cancer
|
|
Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-N3806
-
-
- HY-128774
-
|
AM-6494
|
Beta-secretase
|
Neurological Disease
|
|
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM).
|
-
- HY-B0124
-
|
Zonisamide
AD 810; CI 912
|
Carbonic Anhydrase
Calcium Channel
Sodium Channel
|
Neurological Disease
|
|
Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease.
|
-
- HY-114158A
-
|
Pronase E (Activity ≥ 4000 U/mg)
Pronase (Activity ≥ 4000 U/mg)
|
Others
|
Others
|
|
Pronase E (Activity ≥ 4000 U/mg) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-W014622
-
|
CRT0044876
|
DNA/RNA Synthesis
|
Cancer
|
|
CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds.
|
-
- HY-100954
-
-
- HY-111558A
-
|
Bobcat339 hydrochloride
|
DNA Methyltransferase
|
Cancer
|
|
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
-
- HY-B0815
-
|
Chlorpyrifos
|
AChE
|
Neurological Disease
|
|
Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
|
-
- HY-130516
-
|
Cdc7-IN-4
|
CDK
|
Cancer
|
|
Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-N7450
-
-
- HY-130519
-
|
Cdc7-IN-7
|
CDK
|
Cancer
|
|
Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-N2574
-
|
Gitogenin
|
Glucosidase
|
Metabolic Disease
|
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
|
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-114158
-
|
Pronase E (Activity ≥ 7000 U/g)
Pronase (Activity ≥ 7000 U/g)
|
Others
|
Others
|
|
Pronase E (Activity ≥ 7000 U/g) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-U00373
-
-
- HY-N0548
-
|
α-Angelica lactone
|
Gutathione S-transferase
|
Cancer
|
|
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes.
|
-
- HY-123561
-
|
MMV008138
|
Parasite
|
Infection
|
|
MMV008138 is a species-selective IspD (enzyme 2-C-methyl-d-erythritol 4-phosphate cytidylyltransferase)-targeting antimalarial agent, with an IC50 of 44 nM for PfIspD (P. falciparum IspD). MMV008138 inhibits the growth of P. falciparum Dd2 strain with an IC50 of 250 nM.
|
-
- HY-109785A
-
|
(R)-Gyramide A hydrochloride
|
|
Infection
|
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-116090
-
|
Conoidin A
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-131275
-
|
Imatinib Impurity E
|
Others
|
Others
|
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-N0492
-
-
- HY-N2298
-
|
Camellianin A
|
Apoptosis
|
Cancer
|
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
|
-
- HY-17614
-
|
Ezutromid
SMT C1100; BMN 195; VOX-C1100
|
Others
|
Others
|
|
Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM.
|
-
- HY-107910
-
|
Hyaluronidase
Hyaluronate 4-glycAnohydrolase; Hyaluronoglucosaminidase
|
Others
|
Others
|
|
Hyaluronidase (Hyaluronate 4-glycanohydrolase; Hyaluronoglucosaminidase) is a naturally occurring enzyme that depolymerizes hyaluronic acid by cleavage of glycosidic bonds and has been utilized in ophthalmic surgery.
|
-
- HY-W040073
-
|
Nifurtimox
|
Parasite
Lactate Dehydrogenase
|
Cancer
Infection
|
|
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
|
-
- HY-113081
-
|
1-Methyladenosine
|
Endogenous Metabolite
|
Others
|
|
1-Methyladenosine is an RNA modification originating essentially from two different reaction types, one catalyzed by enzymes and the other the result of the reaction of RNA with certain alkylating agents.
|
-
- HY-W011391
-
|
GPNA hydrochloride
|
Apoptosis
|
Cancer
|
|
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
|
-
- HY-124679
-
|
DS86760016
|
Bacterial
|
Infection
|
|
DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC50s of 0.38, 0.62, and 0.16 μM, respectively.
|
-
- HY-119737
-
|
Chlorsulfuron
|
Others
|
Metabolic Disease
|
|
Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase.
|
-
- HY-109066
-
-
- HY-P1244A
-
-
- HY-P2329
-
-
- HY-B2193
-
|
α-Amylase
|
Others
|
Others
|
|
α-Amylase is a hydrolase enzyme that catalyses the hydrolysis of internal α-1, 4-glycosidic linkages in starch to yield products like glucose and maltose.
|
-
- HY-B0368
-
|
Captopril
SQ 14225
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
|
-
- HY-129039
-
|
Butyrolactone 3
|
Histone Acetyltransferase
|
Cancer
|
|
Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)
|
-
- HY-133116
-
|
4-Hydroxyatomoxetine
|
Others
|
Neurological Disease
|
|
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
|
-
- HY-18767
-
|
Ivosidenib
AG-120
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
Metabolic Disease
|
|
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
|
-
- HY-101930B
-
|
(R)-BMS-816336
|
Others
|
Metabolic Disease
|
|
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
|
-
- HY-B0329
-
|
Isoniazid
INH; Isonicotinic acid hydrazide; Isonicotinic hydrazide
|
Bacterial
Autophagy
Mitophagy
|
Infection
|
|
Isoniazid (INH) is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity.
|
-
- HY-125112
-
-
- HY-N6805
-
|
Isoeugenol acetate
Acetyl isoeugenol
|
AChE
|
Cancer
Inflammation/Immunology
|
|
Isoeugenol acetate (Acetyl isoeugenol), an essential oil constituent of nutmeg, clove, and cinnamon, shows excellent inhibitory effects against some metabolic enzymes such as acetylcholinesterase (AChE) enzymes (IC50=77 nM; Ki=16 nM), α-glycosidase (IC50=19.25 nM; Ki=21 nM), and α-amylase (IC50=411.5 nM). Isoeugenol acetate is used medical and cosmetics industries for its antioxidant, anticancer, antimicrobial and anti-inflammatory properties.
|
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-N2266
-
-
- HY-W016813
-
|
trans-Aconitic acid
|
Endogenous Metabolite
|
Others
|
|
trans-Aconitic acid is present in normal human urine, and it has been suggested that is present in larger amounts with Reye's syndrome and organic aciduria. trans-Aconitic acid is a substrate of enzyme trans-aconitate 2-methyltransferase.
|
-
- HY-18341B
-
|
L-Thyroxine sodium
Levothyroxine sodium; T4 sodium
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
L-Thyroxine sodium (Levothyroxine sodium) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4).
|
-
- HY-N0240
-
|
Herbacetin
|
Others
|
Cancer
|
|
Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
|
-
- HY-12975
-
|
AZ6102
|
PARP
|
Cancer
|
|
AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.
|
-
- HY-111551
-
|
FT113
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo.
|
-
- HY-A0004
-
|
Decitabine
5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716
|
DNA Methyltransferase
Apoptosis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
|
-
- HY-I0736
-
|
Isonicotinic acid
|
Drug Metabolite
Endogenous Metabolite
|
Others
|
|
Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochrome P450 (CYP) enzymes, e.g., CYP2C.
|
-
- HY-123931
-
|
ZLDI-8
|
Notch
Phosphatase
Apoptosis
|
Cancer
|
|
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
|
-
- HY-13233A
-
|
Talabostat mesylate
Val-boroPro mesylate; PT100 mesylate
|
Dipeptidyl Peptidase
|
Cancer
Inflammation/Immunology
|
|
Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
|
-
- HY-13233
-
|
Talabostat
Val-boroPro; PT100
|
Dipeptidyl Peptidase
|
Cancer
Inflammation/Immunology
|
|
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
|
-
- HY-103046
-
|
UbcH5c-IN-1
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
|
-
- HY-100864
-
|
mPGES1-IN-3
|
PGE synthase
|
Inflammation/Immunology
|
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM).
|
-
- HY-129491
-
|
O-Desmethyl Midostaurin
CGP62221; O-Desmethyl PKC412
|
PKC
|
Cancer
|
|
O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
|
-
- HY-W010342
-
|
6-Aminonicotinamide
|
Others
|
Cancer
|
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.
|
-
- HY-126237
-
|
Acetyllovastatin
|
Fungal
|
Infection
|
|
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines.
|
-
- HY-18341
-
-
- HY-W012708
-
-
- HY-119989
-
|
Cyclopyrimorate
|
Others
|
Infection
|
|
Cyclopyrimorate, a highly effective bleaching herbicide for weed control in rice fields, targets homogentisate solanesyltransferase (HST). HST is a downstream enzyme of 4-hydroxyphenylpyruvate dioxygenase in the plastoquinone (PQ) biosynthesis pathway.
|
-
- HY-N6798
-
|
Myriocin
|
HCV
Antibiotic
|
Infection
|
|
Myriocin, a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia, is a potent inhibitor of serine-palmitoyl-transferase (SPT) and a key enzyme in de novo synthesis of sphingolipids. Myriocin strongly suppresses replication of both the subgenomic HCV-1b replicon and the JFH-1 strain of genotype 2a infectious HCV, with an IC50 of 3.5 µg/mL for inhibiting HCV infection.
|
-
- HY-B1776
-
|
Spermidine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Spermidine maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine significantly decreases the H2O2 and O2 .- contents.
|
-
- HY-18341A
-
-
- HY-13332
-
|
Calcifediol-D6
|
VD/VDR
|
Metabolic Disease
|
|
Calcifediol-D6 is the deuterated form of Calcifediol(25-hydroxy Vitamin D3), which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 (cholecalciferol) by the enzyme cholecalciferol 25-hydroxylase.
|
-
- HY-B1776A
-
|
Spermidine trihydrochloride
|
Others
|
Metabolic Disease
|
|
Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2 .- contents.
|
-
- HY-N7072
-
-
- HY-W014316
-
|
5-Bromo-5-nitro-1,3-dioxane
|
Bacterial
Fungal
|
Infection
|
|
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol.
|
-
- HY-109015
-
|
Tucidinostat
Chidamide; HBI-8000; CS 055
|
HDAC
|
Cancer
|
|
Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
|
-
- HY-117048
-
|
PF-4191834
PF-04191834
|
Lipoxygenase
|
Inflammation/Immunology
|
|
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
|
-
- HY-117318
-
|
PDE12-IN-1
|
Phosphodiesterase (PDE)
|
Infection
|
|
PDE12-IN-1 is a potent and selective PDE12 inhibitor with a pIC50 value for enzyme inhibition of 9.1. PDE12-IN-1 increases 2′,5′-linked adenylate polymers (2-5A) levels, and the pEC50 value is 7.7. PDE12-IN-1 shows antiviral activity.
|
-
- HY-13610A
-
-
- HY-122445
-
-
- HY-109052
-
|
Atabecestat
JNJ-54861911
|
Beta-secretase
|
Neurological Disease
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.
|
-
- HY-16903
-
|
PKC-IN-1
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-N0074
-
|
Byakangelicol
|
COX
|
Inflammation/Immunology
|
|
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
|
-
- HY-100487
-
|
TAK-243
MLN7243
|
E1/E2/E3 Enzyme
NF-κB
Apoptosis
|
Cancer
|
|
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
|
-
- HY-W020033
-
|
Lanosterol
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases.
|
-
- HY-N2010
-
-
- HY-N2278
-
|
Kushenol A
LeachiAnone E
|
Tyrosinase
Glucosidase
|
Cancer
|
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
|
-
- HY-13205
-
|
Belnacasan
VX-765
|
Caspase
|
Inflammation/Immunology
|
|
Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
|
-
- HY-13811
-
|
NSC697923
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
|
-
- HY-N3807
-
|
Enniatin B1
|
Acyltransferase
ERK
NF-κB
|
Cancer
Infection
Cardiovascular Disease
|
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
|
-
- HY-120179A
-
|
LP-922761 hydrate
|
Others
|
Neurological Disease
|
|
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
|
-
- HY-113846
-
|
CMP-5 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-120179
-
|
LP-922761
|
Others
|
Neurological Disease
|
|
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
|
-
- HY-107981
-
|
LSN 3213128
|
Antifolate
|
Cancer
|
|
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.
|
-
- HY-107420
-
|
AY 9944
|
Others
|
Metabolic Disease
|
|
AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol.
|
-
- HY-108347
-
|
CP-100356 hydrochloride
|
P-glycoprotein
BCRP
|
Metabolic Disease
|
|
CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM).
|
-
- HY-108476
-
|
INDY
|
DYRK
|
Cancer
|
|
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.
|
-
- HY-134205A
-
|
CBR-470-1
|
Keap1-Nrf2
|
Metabolic Disease
Neurological Disease
|
|
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
|
-
- HY-N7088
-
|
Raffinose
Melitose
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Raffinose (Melitose), a non-digestible short-chain oligosaccharide, is a trisaccharide composed of galactose, glucose, and fructose and can be found in many plants. Raffinose (Melitose) can be hydrolyzed to D-galactose and sucrose by the enzyme α-galactosidase (α-GAL).
|
-
- HY-B0030
-
|
D-Cycloserine
|
iGluR
Bacterial
Antibiotic
|
Infection
Neurological Disease
|
|
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
|
-
- HY-N6840
-
|
Xylotetraose
|
Others
|
Others
|
|
Xylotetraose is a hydrolysis product of Xylan. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose. Xylotetraose can be used for enzyme biochemical analysis.
|
-
- HY-108751
-
|
Aripiprazole Lauroxil
|
Others
|
Neurological Disease
|
|
Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.
|
-
- HY-N7698B
-
|
Hexa-N-acetylchitohexaose
|
Others
|
Cancer
Inflammation/Immunology
|
|
Hexa-N-acetylchitohexaose is an inducer of disease resistance in crop plants, which could elicit an increase of lignification-related and antioxidative enzymes in soybean plants. Hexa-N-acetylchitohexaose is a substrate of lysozyme. Hexa-N-acetylchitohexaose shows antitumor effect.
|
-
- HY-113478
-
|
3β-Ursodeoxycholic acid
Isoursodeoxycholic acid
|
Others
|
Metabolic Disease
|
|
3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) is a bile acid. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) shows good tolerance and well intestinal absorption by oral adminstation. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) can be isomerized by intestinal and hepatic enzymes to yield UDCA.
|
-
- HY-120137
-
|
CMP-5
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-12501A
-
|
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-13240
-
|
LY2886721
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
|
-
- HY-W002585
-
|
O6-Benzylguanine
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.
|
-
- HY-N1510
-
|
Kaempferol 3-O-gentiobioside
|
Glucosidase
|
Metabolic Disease
|
|
Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM.
|
-
- HY-13755A
-
|
(R)-Sulforaphane
L-SulforaphAne
|
Others
|
Cancer
|
|
(R)-Sulforaphane (L-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.
|
-
- HY-12501
-
|
ITI-214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-113089
-
|
Epsilon-(gamma-glutamyl)-lysine
H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys
|
Others
|
Metabolic Disease
|
|
Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration.
|
-
- HY-14280A
-
|
Entacapone sodium salt
|
COMT
|
Neurological Disease
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-14280
-
|
Entacapone
|
COMT
|
Neurological Disease
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-113410
-
|
3-Methylglutaric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
3-Methylglutaric acid, a leucine metabolite, is a conspicuous C6 dicarboxylic organic acid classically associated with two distinct leucine pathway enzyme deficiencies, 3-hydroxy-3-methylglutaryl CoA lyase (HMGCL) and 3-methylglutaconyl CoA hydratase (AUH).
|
-
- HY-17567C
-
|
Heparin sodium salt (MW 15kDa)
Sodium heparin (MW 15kDa); Sodium heparinate (MW 15kDa)
|
Thrombin
Factor Xa
Autophagy
|
Cardiovascular Disease
|
|
Heparin sodium salt (MW 15kDa) (Sodium heparin (MW 15kDa)) is a polymer of Heparin with the molecular weight of 15kDa. Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.
|
-
- HY-128206
-
|
I3MT-3
HMPSNE
|
Hippo (MST)
|
Metabolic Disease
|
|
I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.
|
-
- HY-136528
-
|
RA-9
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
|
-
- HY-14393
-
|
Emodin
FrAngula emodin
|
SARS-CoV
Casein Kinase
Autophagy
|
Cancer
|
|
Emodin (Frangula emodin), an anthraquinone derivative isolated from genus Rheum and Polygonum, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
|
-
- HY-N0157
-
|
Orotic acid
6-Carboxyuracil; Vitamin B13
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats.
|
-
- HY-B0617A
-
|
S-Adenosyl-L-methionine tosylate
S-Adenosyl methionine tosylate; Ademetionine tosylate; AdoMet tosylate
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
S-Adenosyl-L-methionine tosylate (S-Adenosyl methionine tosylate) is produced endogenously from methionine and ATP by action of the enzyme methionine adenosyltransferase and is an important orally active methyl group donor. S-Adenosyl-L-methionine tosylate is a dietary supplement with potent antidepressant and analgesic effects, and has the potential for liver disease and osteoarthritis research.
|
-
- HY-N0157A
-
|
Orotic acid zinc
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (zinc), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid (zinc) is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid (zinc) can induce hepatic steatosis and hepatomegaly in rats.
|
-
- HY-B0617
-
|
S-Adenosyl-L-methionine
S-Adenosyl methionine; Ademetionine; AdoMet
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
S-Adenosyl-L-methionine (S-Adenosyl methionine) is produced endogenously from methionine and ATP by action of the enzyme methionine adenosyltransferase and is an important orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant and analgesic effects, and has the potential for liver disease and osteoarthritis research.
|
-
- HY-14250
-
|
PF-998425
|
Androgen Receptor
|
Endocrinology
|
|
PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research.
|
-
- HY-13522
-
|
Fimepinostat
CUDC-907
|
PI3K
HDAC
Apoptosis
|
Cancer
|
|
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
|
-
- HY-12390
-
|
Lofepramine
Lopramine
|
Others
|
Neurological Disease
|
|
Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties.
|
-
- HY-N2449
-
|
(±)-Licarin A
(±)-trAns-Dehydrodiisoeugenol
|
Parasite
|
Infection
|
|
(±)-Licarin A ((±)-trans-Dehydrodiisoeugenol) is a dihydrobenzofuran neolignan, the resultant of an oxidative coupling reaction of isoeugenol and horseradish peroxidase (HRP) enzyme. (±)-Licarin A displays 58.7% parasite lysis and has an IC50 value of 100.8 µM for trypanocidal activity against trypomastigote forms of T. cruzi. And (±)-Licarin A shows 100% parasites mortality at 200 µM.
|
-
- HY-W007376
-
|
Indole-3-carboxaldehyde
3-Formylindole
|
Others
|
Others
|
|
Indole-3-carboxaldehyde (3-Formylindole), a cabbage extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin.
|
-
- HY-P1141
-
|
GLP-1(9-36)amide
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor.
|
-
- HY-108512
-
|
PD 144418
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity.
|
-
- HY-100014
-
|
KDM5A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
|
-
- HY-P1141A
-
|
GLP-1(9-36)amide TFA
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor.
|
-
- HY-108512A
-
|
PD 144418 oxalate
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.
|
-
- HY-P1792
-
|
Angiotensin II (1-4), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
|
Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-N7434
-
|
N-Nitrosodiethylamine
|
DNA/RNA Synthesis
|
Cancer
|
|
N-Nitrosodiethylamine is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
|
-
- HY-129491S
-
|
O-Desmethyl Midostaurin-d5
CGP62221-d5; O-Desmethyl PKC412-d5
|
Others
|
Cancer
|
|
O-Desmethyl PKC412-d5 (CGP62221-d5) is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism.
|
-
- HY-120944
-
|
BAY-7598
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-117427
-
|
D5D-IN-326
|
Others
|
Metabolic Disease
|
|
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.
|
-
- HY-P1792A
-
|
Angiotensin II (1-4), human TFA
|
Angiotensin Receptor
|
Endocrinology
Metabolic Disease
|
|
Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-135390
-
|
Hydroxy desmethyl Bosentan
Ro 64-1056
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension.
|
-
- HY-119726
-
|
Fosmanogepix
APX001; E1211
|
Fungal
|
Infection
|
|
Fosmanogepix (APX001) is a first-in-class and orally available broad-spectrum antifungal agent, which targets the highly conserved Gwt1 fungal enzyme. Fosmanogepix (APX001) is an N-phosphonooxymethyl prodrug which is rapidly and completely metabolized by systemic alkaline phosphatases to the active moiety, APX001A. Fosmanogepix (APX001) can be used in development for the treatment of invasive fungal infections.
|
-
- HY-12379
-
|
NS-2028
|
Guanylate Cyclase
|
Inflammation/Immunology
|
|
NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM. NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM. NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.
|
-
- HY-13543
-
|
Tretazicar
CB 1954
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
|
-
- HY-12404
-
|
Diminazene aceturate
Diminazene diaceturate
|
Parasite
Angiotensin-converting Enzyme (ACE)
|
Infection
Inflammation/Immunology
|
|
Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties.
|
-
- HY-W011727A
-
|
Pyridoxal 5'-phosphate monohydrate
Pyridoxal phosphate monohydrate
|
Others
|
Neurological Disease
|
|
Pyridoxal 5'-phosphate hydrate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate hydrate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′‐phosphate (PMP).
|
-
- HY-15697
-
|
TUG-770
|
GPR40
|
Metabolic Disease
|
|
TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research.
|
-
- HY-N6802
-
|
Tigloylgomisin H
|
Others
|
Cancer
|
|
Tigloylgomisin H is a lignan isolated from the fruits of S. chinensis, can induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. Tigloylgomisin H functions as a monofunctional inducer that specifically upregulates phase II detoxification enzyme NQO1 through the NF-E2-related factor 2 (Nrf2)-ARE pathway, thus represents a potential liver cancer prevention agent.
|
-
- HY-N0385
-
|
Gomisin J
|
AMPK
Calcium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Gomisin J is a small molecular weight lignan found in Schisandra chinensis and has been demonstrated to have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca 2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells. gomisin J has potential benefits in treating nonalcoholic fatty liver disease.
|
-
- HY-N6851
-
|
Glycyrrhetic acid 3-O-β-D-glucuronide
|
Others
|
Inflammation/Immunology
|
|
Glycyrrhetic acid 3-O-β-D-glucuronide, isolated from glycyrrhiza, is an important derivative of glycyrrhizin (GL) with an anti -allergic activity. Glycyrrhetic acid 3-O-β-D-glucuronide (GAMG) shows that β‐glucuronidases (β‐GUS) are key GAMG-producing enzymes, displaying a high potential to convert GL directly into GAMG.Glycyrrhetic acid 3-O-β-D-glucuronide is valuable as a sweetener.
|
-
- HY-122818
-
|
bpV(phen) trihydrate
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-111191
-
|
ONO-2952
|
Others
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
|
-
- HY-107625A
-
|
SNAP 94847 hydrochloride
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-107625
-
|
SNAP 94847
|
MCHR1 (GPR24)
|
Neurological Disease
Endocrinology
|
|
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-N2118
-
|
Bilobetin
|
PPAR
PKA
|
Metabolic Disease
|
|
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
|
-
- HY-119109
-
|
Laminaran
|
Others
|
Cancer
|
|
Laminaran is an β-1-3-glucan and a typical ligand for Dectin-1 isolated from the brown alga D. dichotoma, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
|
-
- HY-113402A
-
|
Gamma-glutamylcysteine TFA
γ-Glutamylcysteine TFA
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Gamma-glutamylcysteine (γ-Glutamylcysteine) TFA, an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine TFA also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β). Gamma-glutamylcysteine TFA attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes.
|
-
- HY-122815
-
|
Fusicoccin
Fusicoccin A
|
Apoptosis
|
Cancer
|
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
|
-
- HY-W010706
-
|
N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine
5'-O-DMT-N4-Bz-dC
|
Others
|
Others
|
|
N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine (5'-O-DMT-N4-Bz-dC) can be used for synthesis oligodeoxynucleotides containing a 3'-S-phosphorothiolate (3'-PS) linkage. N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine is an useful tool for probing enzyme-catalyzed cleavage processes in DNA.
|
-
- HY-15568A
-
|
A-317491 sodium salt hydrate
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- HY-15568
-
|
A-317491
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- HY-137471
-
|
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-131344
-
|
mTOR inhibitor-8
|
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-136123
-
|
Tubulin inhibitor 8
|
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
-
|
Tubulin inhibitor 7
|
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.
|
-
- HY-136121
-
|
Tubulin inhibitor 6
|
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.
|
-
- HY-112851
-
-
- HY-112812
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
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-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-112722
-
-
- HY-137497
-
|
KRAS inhibitor-9
|
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-101275
-
-
- HY-13278A
-
-
- HY-111370
-
|
mTOR inhibitor-2
|
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-119369
-
-
- HY-111412
-
-
- HY-21141
-
|
Cysteine protease inhibitor-2
|
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-17541A
-
-
- HY-17541
-
-
- HY-112914
-
-
- HY-70005
-
-
- HY-130260
-
-
- HY-128703
-
-
- HY-10442
-
-
- HY-138295
-
|
KRAS inhibitor-10
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 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-12186
-
|
3-Deazaneplanocin A hydrochloride
DZNep hydrochloride; NSC 617989 hydrochloride; 3-DeazAneplAnocin hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
|
-
- HY-112807
-
|
SGLT inhibitor-1
|
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-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-B0385
-
-
- HY-32015
-
|
Cot inhibitor-1
|
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-P0017
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- HY-115514A
-
|
BRK inhibitor P21d hydrochloride
|
Others
|
Cancer
|
|
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
|
-
- HY-128859
-
|
EMT inhibitor-2
|
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-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
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.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-128917
-
-
- HY-15182
-
-
- HY-112474
-
-
- HY-119372
-
-
- HY-13662
-
-
- HY-13662A
-
-
- HY-128617
-
|
Legumain inhibitor 1
|
Others
|
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-119937
-
-
- HY-15253
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
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-122723
-
|
GOT1 inhibitor-1
|
Others
|
Cancer
|
|
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent 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-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135864
-
|
KRAS inhibitor-6
|
Ras
|
Cancer
|
|
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
|
-
- HY-135866
-
|
KRAS inhibitor-8
|
Ras
|
Cancer
|
|
KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
|
-
- HY-135826
-
|
Necroptosis-IN-1
|
RIP kinase
|
Cancer
|
|
Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
|
-
- HY-111408
-
-
- HY-N2033
-
-
- HY-100463
-
-
- HY-135865
-
|
KRAS inhibitor-7
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
|
-
- HY-112607
-
|
Tubulin inhibitor 1
|
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-124798
-
-
- HY-32018
-
|
Cot inhibitor-2
|
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-118810
-
-
- HY-B0884
-
-
- HY-112569
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-112906
-
-
- HY-50856A
-
-
- HY-104022
-
-
- HY-117262
-
-
- HY-U00410
-
-
- HY-13276
-
-
- HY-B0218
-
-
- HY-106067A
-
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-17542
-
|
PLpro inhibitor
|
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-126328
-
|
PKC-theta inhibitor 1
|
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-15760
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-13662B
-
|
(R)-Lansoprazole
DexlAnsoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-131705
-
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-15183
-
-
- HY-U00387
-
-
- HY-107986
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-N0565A
-
-
- HY-108322
-
-
- HY-112270
-
-
- HY-50880
-
-
- HY-N2221
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-15604A
-
-
- HY-112269
-
-
- HY-128723
-
-
- HY-50879
-
-
- HY-104032
-
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-50900
-
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-16569
-
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-W008923
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-101791
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-16657
-
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-119808
-
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-P2478
-
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-15358
-
|
ALK inhibitor 2
|
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-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-15357
-
|
ALK inhibitor 1
|
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-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-12072
-
|
Lck Inhibitor
|
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-P1398
-
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-10846
-
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-10451S
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N2219
-
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-112913
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-114309
-
-
- HY-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859A
-
|
Zidebactam sodium salt
WCK-5107 sodium salt
|
Bacterial
|
Infection
|
|
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-118355
-
|
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-126331
-
-
- HY-12824
-
|
RNPA1000
|
Antibiotic
Bacterial
|
Infection
|
|
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethAnolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Infection
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-N1447
-
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-15842
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-D0886
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-B2007
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
-
-
- HY-19707
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100456
-
-
- HY-111493
-
-
- HY-50706A
-
|
Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-125997
-
|
BTK inhibitor 10
|
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-13228
-
-
- HY-126288
-
|
ERK1/2 inhibitor 2
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
|
-
- HY-16062
-
|
ARQ 621
|
Kinesin
|
Cancer
|
|
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
|
-
- HY-119935
-
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-N8533
-
|
Sodium Camptothecin
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA.
|
-
- HY-13985
-
-
- HY-12031A
-
-
- HY-U00453
-
-
- HY-112910
-
|
Grp94 Inhibitor-1
|
HSP
|
Cancer
Infection
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
|
-
- HY-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- HY-13984
-
|
Mutant EGFR inhibitor
|
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-22166
-
-
- HY-W047428
-
-
- HY-112451
-
-
- HY-U00377
-
-
- HY-15217
-
-
- HY-15859
-
|
Atglistatin
|
ATGL
|
Metabolic Disease
|
|
Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.
|
-
- HY-77521
-
-
- HY-13502
-
-
- HY-119938
-
-
- HY-70027A
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-128962
-
-
- HY-13278
-
-
- HY-13060
-
-
- HY-101474
-
|
(±)-Zanubrutinib
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
|
-
- HY-124594
-
-
- HY-19731
-
-
- HY-101462
-
-
- HY-B0902A
-
|
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-101963
-
-
- HY-115213
-
-
- HY-70073
-
-
- HY-15775
-
-
- HY-13502A
-
-
- HY-70003
-
-
- HY-112720
-
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
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-100932A
-
|
ML-9 Free Base
|
Myosin
|
Cancer
|
|
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-135318
-
|
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-100816
-
|
Rbin-1
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-100556
-
|
Tie2 kinase inhibitor 1
|
Others
|
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-112715
-
-
- HY-14165
-
-
- HY-124793A
-
|
GAK inhibitor 49 hydrochloride
|
Others
|
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-19727A
-
-
- HY-129167
-
-
- HY-128918
-
|
SIS17
|
HDAC
|
Others
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
|
-
- HY-124793
-
|
GAK inhibitor 49
|
Others
|
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-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
|
Suramin
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-P0081
-
-
- HY-133110
-
|
Afatinib N-Oxide
|
Others
|
Others
|
|
Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
|
-
- HY-15798
-
-
- HY-114418
-
-
- HY-N5038
-
|
Mauritianin
|
Topoisomerase
|
Cancer
|
|
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.
|
-
- HY-13606
-
|
Dacinostat
NVP-LAQ824; LAQ824
|
HDAC
Autophagy
|
Cancer
|
|
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
|
-
- HY-13256
-
-
- HY-P1452A
-
-
- HY-Y0882
-
-
- HY-16420
-
|
R112
|
Syk
|
Inflammation/Immunology
|
|
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
|
-
- HY-111919
-
-
- HY-15588
-
-
- HY-B0830
-
|
Isoprocarb
|
AChE
|
Neurological Disease
|
|
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
|
-
- HY-N1502
-
|
Carboxyatractyloside
Gummiferin
|
Others
|
Cancer
|
|
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.
|
-
- HY-12054A
-
-
- HY-114423
-
-
- HY-16931
-
|
SMIFH2
|
Others
|
Cancer
|
|
SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton.
|
-
- HY-10809
-
|
Bitopertin
RG1678; RO4917838
|
GlyT
|
Neurological Disease
|
|
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-19609
-
-
- HY-131268
-
-
- HY-N6619A
-
|
Lycoramine
|
AChE
|
Neurological Disease
|
|
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
|
-
- HY-104028
-
-
- HY-12814A
-
-
- HY-12814
-
|
TH588
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
- HY-111506
-
-
- HY-12420
-
|
JNJ-47117096 hydrochloride
MELK-T1 hydrochloride
|
MELK
FLT3
|
Cancer
|
|
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
|
-
- HY-16982
-
|
Cercosporamide
(-)-Cercosporamide
|
Fungal
MNK
|
Cancer
Infection
|
|
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
|
-
- HY-136347
-
-
- HY-13280
-
-
- HY-18928
-
|
FAK inhibitor 5
|
FAK
|
Cancer
|
|
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
|
-
- HY-N4186
-
-
- HY-103002
-
|
SU5408
VEGFR2 Kinase Inhibitor I
|
VEGFR
|
Cardiovascular Disease
|
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
|
-
- HY-B0497B
-
-
- HY-131446
-
|
Chk1-IN-5
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
|
-
- HY-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-117491
-
-
- HY-124416
-
|
ML604086
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
|
-
- HY-103490
-
|
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
|
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
|
-
- HY-17367A
-
|
Atazanavir sulfate
BMS-232632 sulfate
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Cancer
Infection
|
|
Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-122866
-
|
ZT-12-037-01
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
|
-
- HY-109574
-
|
Raf inhibitor 2
|
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-100227
-
|
E 64c
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-66004
-
|
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-115502
-
|
BCI
(E)-BCI
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
|
-
- HY-80003
-
|
QL47
|
Btk
|
Cancer
Infection
|
|
QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC50 of 7 nM.
|
-
- HY-133019
-
-
- HY-P1045
-
|
187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-124653
-
|
HSP27 inhibitor J2
J2
|
HSP
|
Cancer
|
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
|
-
- HY-P1045A
-
|
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA 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 TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-15766A
-
|
GNE-617 hydrochloride
|
NAMPT
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-12399
-
|
MKC9989
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-112280
-
-
- HY-10247
-
|
BRAF inhibitor
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-12726A
-
-
- HY-N2522
-
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-108820
-
-
- HY-108817
-
-
- HY-13452
-
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-10162S
-
-
- HY-U00370
-
-
- HY-111489A
-
-
- HY-17421A
-
-
- HY-135383A
-
-
- HY-128977
-
-
- HY-12000
-
|
AG490
Tyrphostin AG490; Tyrphostin B42
|
EGFR
STAT
JAK
Autophagy
|
Cancer
|
|
AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
|
-
- HY-A0122
-
-
- HY-111446
-
-
- HY-17381
-
-
- HY-N6031
-
|
Dendrophenol
|
NF-κB
|
Cancer
|
|
Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.
|
-
- HY-Y0172
-
-
- HY-13026S
-
|
Idelalisib D5
CAL-101 D5; GS-1101 D5
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor.
|
-
- HY-108941
-
|
Salicyl-AMS
|
Bacterial
|
Infection
|
|
Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
|
-
- HY-15282
-
-
- HY-B0806
-
|
Proguanil
|
Parasite
Antifolate
|
Infection
|
|
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
|
-
- HY-N2597
-
-
- HY-B0806A
-
-
- HY-112297
-
-
- HY-13420
-
-
- HY-100736
-
|
ML348
GNF-Pf-1127
|
Phospholipase
|
Cancer
|
|
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
|
-
- HY-15202
-
|
Binimetinib
MEK162; ARRY-162; ARRY-438162
|
MEK
Autophagy
|
Cancer
|
|
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
|
-
- HY-102007
-
|
Gamitrinib TPP
|
HSP
|
Cancer
|
|
Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-12726
-
-
- HY-N1724
-
-
- HY-15766
-
|
GNE-617
|
NAMPT
|
Metabolic Disease
Cancer
|
|
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-111489B
-
-
- HY-126253
-
|
BI-4916
|
Others
|
Cancer
|
|
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor.
|
-
- HY-136485
-
-
- HY-B1863
-
|
Iprobenfos
|
Fungal
|
Infection
|
|
Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.
|
-
- HY-135899
-
|
SIRT7 inhibitor 97491
|
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-B2145
-
|
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-107412
-
|
Proteasome inhibitor IX
PS-IX; AM114
|
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
|
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
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-10255AS
-
|
Sunitinib D10
SU 11248 D10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-124726
-
|
Aumitin
|
Autophagy
|
Cancer
Neurological Disease
|
|
Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
|
-
- HY-19727
-
-
- HY-N7674A
-
|
Angoline hydrochloride
|
STAT
|
Cancer
|
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-P1290
-
|
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-N7674
-
|
Angoline
|
STAT
|
Cancer
|
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-109019
-
|
Vorolanib
CM082; X-82
|
VEGFR
PDGFR
|
Cancer
Cardiovascular Disease
|
|
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
|
-
- HY-12054
-
|
Hesperadin
|
Aurora Kinase
Autophagy
Influenza Virus
Parasite
|
Cancer
|
|
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
|
-
- HY-100734
-
-
- HY-123772
-
|
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-100899
-
-
- HY-101705
-
-
- HY-N6619
-
-
- HY-109877
-
-
- HY-100299
-
-
- HY-P2470
-
-
- HY-B0106
-
-
- HY-50710
-
|
KU-0063794
|
mTOR
|
Cancer
|
|
KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
|
-
- HY-137239
-
-
- HY-100303A
-
|
FR194738
|
Others
|
Metabolic Disease
|
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-50946
-
-
- HY-15886
-
-
- HY-112131
-
-
- HY-19326
-
-
- HY-12971
-
|
Nampt-IN-1
LSN3154567
|
NAMPT
|
Cancer
|
|
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
|
-
- HY-130255
-
-
- HY-101479
-
|
Iclaprim
AR-100
|
Bacterial
|
Infection
|
|
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
|
-
- HY-70027
-
-
- HY-108900A
-
-
- HY-N5118
-
|
Chimonanthine
(-)-ChimonAnthine
|
Tyrosinase
|
Cancer
|
|
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
|
-
- HY-U00049
-
-
- HY-16904
-
|
RI-2
|
RAD51
|
Cancer
|
|
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
|
-
- HY-103036
-
-
- HY-111410
-
-
- HY-10862
-
|
FAAH inhibitor 1
Benzothiazole Analog 3
|
FAAH
Autophagy
|
Cancer
|
|
FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
|
-
- HY-13256A
-
|
Desmethyl Erlotinib
OSI-420 free base; CP-373420
|
Drug Metabolite
|
Cancer
|
|
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.
|
-
- HY-15231
-
-
- HY-15735
-
|
c-Met inhibitor 1
|
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-10997S
-
|
Ibrutinib D5
PCI-32765 D5
|
Btk
|
Cancer
|
|
Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
|
-
- HY-10268S
-
-
- HY-10450S
-
-
- HY-15586
-
|
L67
DNA Ligase Inhibitor
|
DNA/RNA Synthesis
|
Cancer
|
|
L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
|
-
- HY-B0008
-
-
- HY-15288
-
-
- HY-115502A
-
|
BCI hydrochloride
(E)-BCI hydrochloride
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
|
-
- HY-12031
-
-
- HY-136538
-
|
LQZ-7I
|
Survivin
|
Cancer
|
|
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
|
-
- HY-N2006
-
|
Ganoderic acid B
|
HIV Protease
|
Infection
|
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
|
-
- HY-119934
-
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-103359
-
|
Ceranib1
|
Others
|
Cancer
|
|
Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.
|
-
- HY-114169
-
|
WRG-28
|
Discoidin Domain Receptor
|
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
|
-
- HY-16592
-
|
Brefeldin A
BFA; CyAnein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-101664
-
|
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-112373
-
|
Aurora Kinase Inhibitor 3
|
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>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, and several induced structural changes in the active-site compared with other published AIK structures.
|
-
- HY-135396
-
|
(1S,2S)-Bortezomib
|
Proteasome
Apoptosis
|
Cancer
|
|
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
|
-
- HY-136149A
-
|
Mpro inhibitor N3 hemihydrate
|
SARS-CoV
Virus Protease
|
Infection
|
|
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively.
|
-
- HY-13803C
-
|
Tazemetostat hydrobromide
EPZ-6438 hydrobromide; E-7438 hydrobromide
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-13803A
-
|
Tazemetostat trihydrochloride
EPZ-6438 trihydrochloride; E-7438 trihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-122862
-
|
RAS inhibitor Abd-7
|
Ras
|
Cancer
|
|
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V.
|
-
- HY-P1290A
-
|
PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-B0166
-
-
- HY-P0222
-
|
PKI(5-24)
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-114996
-
-
- HY-103032
-
|
Multi-kinase inhibitor 1
|
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-10009
-
-
- HY-Y0445A
-
|
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-66005
-
-
- HY-133014
-
-
- HY-13512
-
|
Camostat mesylate
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
|
-
- HY-122632
-
|
Ciliobrevin D
|
Hedgehog
|
Cancer
|
|
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
|
-
- HY-B0166A
-
|
L-Ascorbic acid sodium salt
Sodium L-ascorbate; Vitamin C sodium salt
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
|
-
- HY-10261S
-
|
Afatinib D6
BIBW 2992 D6
|
EGFR
Autophagy
|
Cancer
|
|
Afatinib D6 (BIBW 2992 D6) is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor.
|
-
- HY-135391
-
-
- HY-B1279A
-
-
- HY-15233
-
|
Letermovir
AIC246
|
CMV
|
Infection
|
|
Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
|
-
- HY-128580
-
|
FAK inhibitor 2
|
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-101053
-
|
Src Inhibitor 1
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-50909
-
|
Perifosine
KRX-0401; NSC 639966; D21266
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
|
-
- HY-101766
-
-
- HY-16510A
-
-
- HY-N0143
-
|
Phlorizin
Floridzin; NSC 2833
|
SGLT
Na+/K+ ATPase
|
Metabolic Disease
|
|
Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na +/K +-ATPase inhibitor.
|
-
- HY-U00096
-
-
- HY-112494
-
-
- HY-B1243
-
-
- HY-32351
-
-
- HY-112491
-
-
- HY-N7089
-
|
Benzoyleneurea
|
Bacterial
|
Infection
|
|
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
|
-
- HY-18931A
-
|
NSC305787 hydrochloride
|
Others
|
Cancer
|
|
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-112432
-
-
- HY-15247
-
-
- HY-N2403
-
-
- HY-16510
-
-
- HY-12357
-
-
- HY-126142
-
-
- HY-112493
-
-
- HY-101464
-
|
ML329
|
Others
|
Others
|
|
ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
|
-
- HY-12682
-
|
Glutaminase C-IN-1
Compound 968
|
Glutaminase
|
Cancer
|
|
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
|
-
- HY-102007A
-
|
Gamitrinib TPP hexafluorophosphate
|
HSP
|
Cancer
|
|
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-100541
-
|
INH6
|
Apoptosis
|
Cancer
|
|
INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
|
-
- HY-32351A
-
-
- HY-100735
-
-
- HY-13067
-
-
- HY-15679
-
-
- HY-19352
-
-
- HY-13062
-
-
- HY-107433
-
-
- HY-126134
-
-
- HY-18931
-
|
NSC305787
|
Others
|
Cancer
|
|
NSC305787 is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-112128
-
-
- HY-15223
-
-
- HY-112492
-
-
- HY-15457
-
-
- HY-100792
-
|
URB602
|
Others
|
Cancer
|
|
URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
|
-
- HY-112164
-
-
- HY-N7452
-
-
- HY-70028
-
-
- HY-111784
-
-
- HY-131002
-
-
- HY-19763
-
|
BEBT-908
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) .
|
-
- HY-18979
-
|
Lactimidomycin
|
Influenza Virus
|
Cancer
Infection
|
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.
|
-
- HY-103194
-
|
KH7
|
Others
|
Others
|
|
KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-133114
-
-
- HY-112800
-
|
cyt-PTPε Inhibitor-1
|
Phosphatase
|
Metabolic Disease
|
|
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
|
-
- HY-112062
-
|
POL1-IN-1
|
DNA/RNA Synthesis
|
Cancer
|
|
POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
|
-
- HY-118532
-
|
Tyrphostin AG30
AG30
|
EGFR
|
Cancer
|
|
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
|
-
- HY-11001
-
|
PHA-793887
|
CDK
Apoptosis
|
Cancer
|
|
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
|
-
- HY-N0149
-
-
- HY-100263
-
-
- HY-N0342
-
-
- HY-101244
-
-
- HY-112870A
-
-
- HY-P0290A
-
-
- HY-100222
-
|
CZ415
|
mTOR
|
Cancer
|
|
CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
|
-
- HY-112907
-
-
- HY-119692
-
|
Curvulin
|
Microtubule/Tubulin
|
Others
|
|
Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.
|
-
- HY-12056
-
|
BIX02189
|
MEK
ERK
|
Cancer
|
|
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
|
-
- HY-12957
-
-
- HY-10367A
-
|
Canertinib dihydrochloride
CI-1033 dihydrochloride; PD-183805 dihydrochloride
|
EGFR
|
Cancer
|
|
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
|
-
- HY-128889
-
-
- HY-135383
-
-
- HY-12204
-
|
PFK-015
|
Autophagy
|
Cancer
|
|
PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.
|
-
- HY-100750
-
-
- HY-112712
-
|
Cyclophilin inhibitor 1
|
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-13577A
-
|
Oclacitinib maleate
PF-03394197 maleate
|
JAK
|
Inflammation/Immunology
|
|
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
|
-
- HY-N3002
-
|
α-Arbutin
4-Hydroxyphenyl α-D-glucopyrAnoside
|
Tyrosinase
|
Metabolic Disease
|
|
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
|
-
- HY-10331S
-
-
- HY-111357
-
|
Antifungal agent 2
|
Fungal
|
Infection
|
|
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.
|
-
- HY-13966
-
|
2-Deoxy-D-glucose
2-DG; 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose
|
Hexokinase
HSV
Apoptosis
|
Cancer
|
|
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.
|
-
- HY-12589
-
-
- HY-126482
-
|
Telomerase-IN-2
|
Telomerase
|
Cancer
|
|
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
|
-
- HY-15162A
-
-
- HY-15417
-
|
ML-7 hydrochloride
|
Myosin
YAP
|
Cancer
|
|
ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
|
-
- HY-12622
-
|
HSP70-IN-1
|
HSP
|
Cancer
|
|
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
|
-
- HY-126292
-
-
- HY-112861A
-
-
- HY-12444
-
|
Y15
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-100852
-
-
- HY-12289A
-
|
Defactinib hydrochloride
VS-6063 hydrochloride; PF 04554878 hydrochloride
|
FAK
|
Cancer
|
|
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
|
-
- HY-W018931
-
-
- HY-12589A
-
-
- HY-115666
-
|
COH34 analog 1
|
Others
|
Cancer
|
|
COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
|
-
- HY-13806
-
|
XL388
|
mTOR
Autophagy
|
Cancer
|
|
XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
|
-
- HY-12744
-
-
- HY-10129
-
|
Veliparib
ABT-888
|
PARP
Autophagy
|
Cancer
|
|
Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
|
-
- HY-14560C
-
|
Reboxetine mesylate
FCE20124 mesylate; PNU155950E mesylate
|
Adrenergic Receptor
|
Neurological Disease
|
|
Reboxetine mesylate (FCE20124 mesylate) is a potent, selective, and specific noradrenaline reuptake inhibitor (NARI) for the research of depression. Reboxetine mesylate inhibits the uptake of norepinephrine, with a Ki of 8 nM.
|
-
- HY-111651
-
-
- HY-N5015
-
|
Rosmanol
|
Others
|
Inflammation/Immunology
Cancer
|
|
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
|
-
- HY-133246
-
-
- HY-10366
-
-
- HY-112445
-
-
- HY-12479A
-
|
Epetraborole hydrochloride
GSK2251052 hydrochloride
|
Bacterial
|
Infection
|
|
Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase".
|
-
- HY-19832
-
|
SC66
|
Akt
Apoptosis
|
Cancer
|
|
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-136110
-
-
- HY-14934
-
|
Rosabulin
STA 5312
|
Microtubule/Tubulin
|
Cancer
|
|
Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity.
|
-
- HY-111451
-
|
ATR inhibitor 1
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 µΜ.
|
-
- HY-115584
-
|
Lufenuron
|
Parasite
|
Infection
|
|
Lufenuron is a lipophilic benzoylurea insecticide and a chitin synthesis inhibitor that can used for flea and fish lice control. Lufenuron inhibits moulting of arthropods.
|
-
- HY-N2182
-
-
- HY-100303
-
-
- HY-135328
-
-
- HY-126146
-
-
- HY-112136
-
|
TAO Kinase inhibitor 1
|
Others
|
Cancer
|
|
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.
|
-
- HY-100374
-
|
Val-Cit-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
|
-
- HY-P0222A
-
|
PKI(5-24) TFA
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-100886
-
|
BAY1082439
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
|
-
- HY-50846
-
|
SCH772984
|
ERK
|
Cancer
|
|
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
|
-
- HY-N0112
-
|
Dihydromyricetin
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Cancer
Infection
|
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-15480
-
|
NSC 42834
JAK2 Inhibitor V; Z3
|
JAK
|
Cancer
|
|
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
|
-
- HY-100126
-
|
Tubercidin
7-Deazaadenosine
|
Bacterial
DNA/RNA Synthesis
Influenza Virus
Antibiotic
|
Infection
|
|
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC50 of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.
|
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-110100
-
|
CPYPP
|
Others
|
Inflammation/Immunology
|
|
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.
|
-
- HY-112701
-
|
CCR6 inhibitor 1
|
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-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-100434
-
|
PD-161570
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cancer
Cardiovascular Disease
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
|
-
- HY-12041
-
|
SP600125
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
|
-
- HY-N2360
-
|
Hinokiflavone
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
|
-
- HY-122727
-
|
STL127705
|
DNA-PK
|
Cancer
|
|
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
|
-
- HY-119375
-
