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Pathways Recommended: Metabolic Enzyme/Protease
Results for "

Enzymes Inhibitors

" in MCE Product Catalog:

535

Inhibitors & Agonists

15

Screening Libraries

1

Fluorescent Dye

13

Peptides

48

Natural
Products

54

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-B1433
    Perindoprilat

    S 9780

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research.
  • HY-108647
    EO 1428

    p38 MAPK Inflammation/Immunology
    EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.
  • HY-129430
    N-Methylprotoporphyrin IX

    Others Others
    N-Methylprotoporphyrin IX is a potent inhibitor of ferrochelatase enzyme.
  • HY-124927
    ARN14988

    Others Cancer
    ARN14988 is a potent inhibitor of acid ceramidase (ACDase) (IC50=12.8 nM for the human enzyme).
  • HY-125965
    BioA-IN-13

    Bacterial Infection
    BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
  • HY-P1044
    Spinorphin

    LVV-hemorphin-4

    Others Neurological Disease
    Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
  • HY-117374
    HDAC3-IN-1

    HDAC Cancer
    HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM.
  • HY-124861
    Malic enzyme inhibitor ME1

    ME1

    Others Cancer Metabolic Disease
    Malic enzyme inhibitor ME1 (ME1; compound 1) is a potent inhibitor of Malic enzyme (ME1) with an IC50 of 0.15 μM.
  • HY-U00459A
    GSK2850163 (S enantiomer)

    IRE1 Others
    GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
  • HY-10827
    Kelatorphan

    Others Neurological Disease
    Kelatorphan is a full inhibitor of enkephalin degrading enzymes.
  • HY-101681
    Utibapril

    FPL 63547

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Utibapril is an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activities.
  • HY-B0263
    Thiabendazole

    2-(4-Thiazolyl)benzimidazole

    Mitochondrial Metabolism Parasite Infection
    Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
  • HY-144800
    FWM-1

    SARS-CoV Infection
    FWM-1 is a potent SARS-COV-2 NSP13 helicase enzyme inhibitor with binding free energy equals -328.6 kcal/mol. FWM-1 effectively disrupts the binding of ATP to the SARS-COV2 helicase enzyme.
  • 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
    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.
  • HY-U00459B
    GSK2850163 hydrochloride

    IRE1 Cancer
    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.
  • HY-108321
    Zofenopril

    Angiotensin-converting Enzyme (ACE) Neurological Disease
    Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
  • HY-U00041
    Pivalopril

    Pivopril; RHC 3659(S)

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Pivalopril is a new orally active angiotensin converting enzyme (ACE) inhibitor.
  • HY-117430
    Hymeglusin

    F-244; 1233A; L-659699

    Antibiotic Cancer Infection Metabolic Disease
    Hymeglusin, as a fungal β-lactone antibiotic, is a HMG-CoA synthase inhibitor (IC50 = 0.12 μM). Hymeglusin covalently modifies the active Cys 129 residue of the enzyme.
  • 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-112862
    Arg-AMS

    Aminoacyl-tRNA Synthetase Others
    Arg-AMS (compound 24) 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-B0655
    Zofenopril calcium

    SQ26991

    Angiotensin-converting Enzyme (ACE) Reactive Oxygen Species Cardiovascular Disease
    Zofenopril Calcium (SQ26991) is an antioxidant that acts as an angiotensin-converting enzyme inhibitor.
  • HY-16450
    SB 204990

    ATP Citrate Lyase Metabolic Disease
    SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
  • HY-116023
    Moveltipril

    Moveltipril calcium; MC-838

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Moveltipril (Moveltipril calcium; MC-838) is a potent angiotensin converting enzyme (ACE) inhibitor.
  • HY-107393
    LY-311727

    Phospholipase Inflammation/Immunology
    LY-311727 is a potent secretory non-pancreatic phospholipase A2 (sPLA2) inhibitor (IC50 <1 μM for group IIA sPLA2). sPLA2 is an important proinflammatory enzyme.
  • HY-P0143
    Leucylarginylproline

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Leucylarginylproline is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 0.27μM.
  • HY-B0279
    Ramipril

    HOE-498

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease Cancer
    Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
  • HY-145652
    AMP-945

    FAK Cancer
    AMP-945 is an inhibitor of the enzyme focal adhesion kinase (FAK).
  • HY-U00074
    Rentiapril racemate

    SA-446 racemate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Rentiapril racemate (SA-446 racemate) is the racemate of Rentiapril. Rentiapril is an angiotensin converting enzyme (ACE) inhibitor.
  • HY-107337
    Delapril hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Delapril hydrochloride is an angiotensin-converting enzyme (ACE) inhibitor for the treatment of cardiovascular diseases.
  • HY-112860
    Asp-AMS

    Aminoacyl-tRNA Synthetase Mitochondrial Metabolism Metabolic Disease
    Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
  • HY-A0116S
    Trandolaprilate D5

    Trandolaprilat D5; RU 44403 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolaprilate D5 is a deuterium labeled Trandolaprilate (Trandolaprilat). Trandolaprilate is an angiotensin-converting enzyme (ACE) inhibitor.
  • HY-144799
    FWM-4

    SARS-CoV Infection
    FWM-4 is a potent SARS-COV-2 NSP13 helicase enzyme inhibitor.
  • HY-W010538
    trans-4-Methylcyclohexanamine

    Parasite Infection
    trans-4-Methylcyclohexanamine is an intermediate and can be used for the development of T. cruzi enzyme inhibitor.
  • HY-B0093
    Benazepril

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Benazepril, an angiotensin converting enzyme inhibitor, which is a medication used to treat high blood pressure.
  • 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
    (±)-WS75624B

    Others Cardiovascular Disease
    (±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL.
  • HY-B1202A
    Alrestatin sodium

    AY-22284A

    Aldose Reductase Endocrinology
    Alrestatin sodium is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.
  • HY-B0331A
    Enalapril maleate

    MK-421 maleate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalapril (maleate) (MK-421 (maleate)), the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor.
  • HY-107582
    JW480

    Others Cancer
    JW480 is a potent and selective inhibitor of a serine hydrolase enzyme KIAA1363.
  • HY-A0043A
    Cilazapril monohydrate

    Ro 31-2848 monohydrate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Cilazapril Monohydrate is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.
  • HY-B0093A
    Benazepril hydrochloride

    CGS14824A

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Benazepril hydrochloride, an angiotensin converting enzyme inhibitor, which is a medication used to treat high blood pressure.
  • HY-A0043
    Cilazapril

    Ro 31-2848

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Cilazapril is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.
  • HY-13989
    b-AP15

    NSC 687852

    Deubiquitinase Apoptosis Cancer
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
  • HY-100615
    Revizinone

    R80122

    Phosphodiesterase (PDE) Cardiovascular Disease
    Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM.
  • HY-18690A
    Enasidenib mesylate

    AG-221 mesylate

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
  • HY-138067
    SSAA09E2

    SARS-CoV Inflammation/Immunology
    SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
  • HY-132884
    TTK inhibitor 3

    Others Cancer
    TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
  • HY-107994
    Aminooxyacetic acid hemihydrochloride

    Carboxymethoxylamine hemihydrochloride; Aminooxyacetate hemihydrochloride

    GABA Receptor Cancer
    Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
  • HY-150621
    AS1134900

    Others Cancer
    AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor.
  • HY-N2021
    Phosphoramidon

    MMP Angiotensin-converting Enzyme (ACE) Neprilysin Endogenous Metabolite Cancer Inflammation/Immunology Cardiovascular Disease
    Phosphoramidon, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively.
  • 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-139566
    Abrucomstat

    3-Nitroxypropanol; 3-NOP

    Others Others
    Abrucomstat (3-Nitroxypropanol) acts as an enzyme inhibitor to decrease ruminal methanogenesis.
  • HY-106446
    Rentiapril

    SA-446

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Rentiapril is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity.
  • HY-16273A
    L-778123 hydrochloride

    L-778,123 hydrochloride

    Farnesyl Transferase Cancer
    L-778123 hydrochloride is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.
  • HY-B0477
    Quinapril hydrochloride

    CI-906

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinapril (hydrochloride) (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications.
  • HY-18948
    GSK321

    Isocitrate Dehydrogenase (IDH) Cancer
    GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia.
  • 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-108285
    (Rac)-Telmesteine

    Others Inflammation/Immunology
    (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-B0882
    Edrophonium chloride

    Cholinesterase (ChE) 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-N7263
    Galanthamine N-Oxide

    Cholinesterase (ChE) 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-N2021A
    Phosphoramidon Disodium

    MMP Angiotensin-converting Enzyme (ACE) Neprilysin Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease Cancer
    Phosphoramidon Disodium, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon Disodium also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, 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-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-124909A
    FR054

    Others Cancer
    FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect.
  • HY-112861
    Gln-AMS

    Aminoacyl-tRNA Synthetase Bacterial Infection
    Gln-AMS is an aminoacyl-tRNA synthetases (AARS) inhibitor, which binds the A-domain within the NRPS enzymes.
  • HY-132824
    Ledaborbactam etzadroxil

    VNRX-7145

    Bacterial Infection
    Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor.
  • 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-132987
    ARX-1796

    AV-006

    Bacterial Infection
    ARX-1796 (AV-006), an Avibactam prodrug, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes.
  • HY-101790
    ZM223

    NEDD8-activating Enzyme Cancer
    ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.
  • HY-121517
    URB754

    Others Neurological Disease
    URB754 is a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) with an IC50 of 200 nM.
  • HY-B0382
    Fosinopril sodium

    SQ28555

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
  • HY-B0331AS
    Enalapril D5 maleate

    MK-421 D5 maleate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalapril (MK-421) D5 maleate is deuterium labeled Enalapril, which is an angiotensin converting enzyme (ACE) inhibitor.
  • HY-18207
    Fasidotril

    Alatriopril

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Fasidotril is a dual inhibitor of neprilysin and angiotensin-converting enzyme (ACE) for the potential treatment of hypertension and congestive heart failure (CHF).
  • HY-107318
    Alacepril

    Cetapril; DU-1219

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Alacepril (Cetapril) is an orally active angiotensin converting enzyme (ACE) inhibitor with long lasting antihypertensive effect.
  • HY-109059
    Fulacimstat

    BAY1142524

    Others Cardiovascular Disease
    Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
  • HY-16437
    RP-64477

    Acyltransferase Cardiovascular Disease
    RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
  • 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-76200
    Voriconazole

    UK-109496

    Fungal Bacterial Infection Cancer
    Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • HY-147365
    Acifluorfen-methyl

    Others Others
    Acifluorfen-methyl is an inhibitor of the heme and chlorophyll biosynthetic enzyme protoporphyrinogen oxidase (Protox). Acifluorfen-methyl is a photobleaching herbicide.
  • 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-13344A
    PF-8380 hydrochloride

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology
    PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
  • HY-B1093
    Fenchlorphos

    Parasite Cholinesterase (ChE) 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
    Valnemulin hydrochloride

    Bacterial Antibiotic Others
    Valnemulin hydrochloride is a pleuromutilin antibiotic which inhibits protein synthesis in bacteria by binding the peptidyl transferase enzyme in the 50s ribosomal subunit.
  • HY-18206
    Lisinopril

    MK-521

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
  • HY-108321S
    Zofenopril-d5

    Angiotensin-converting Enzyme (ACE) Neurological Disease
    Zofenopril-d5 is deuterium labeled Zofenopril. Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
  • HY-13344
    PF-8380

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology
    PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
  • HY-N0125
    Diosmetin

    Cytochrome P450 Cancer
    Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
  • HY-126362
    ML266

    Glucosidase Others
    ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease.
  • HY-76200B
    Voriconazole camphorsulfonate

    UK-109496 camphorsulfonate

    Fungal Bacterial Infection
    Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • 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

    Parasite Infection Cancer
    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
    TAS4464 hydrochloride

    NEDD8-activating Enzyme Cancer
    TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-B0331
    Enalapril

    MK-421

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease Cancer
    Enalapril (MK-421) is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research.
  • HY-B0744A
    Eflornithine hydrochloride

    DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride

    Parasite Infection Cancer
    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-128586
    TAS4464

    NEDD8-activating Enzyme Cancer
    TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  • HY-B0331B
    Enalapril sodium

    MK-421 sodium

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalapril (MK-421) sodium is an angiotensin-converting enzyme (ACE) inhibitor, can be used for hypertensive diseases research.
  • 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. Umibecestat can be used for the research of alzheimer's disease.
  • HY-147730
    HDAC6-IN-8

    HDAC Cancer
    A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
  • HY-33914
    4-Hydroxymethylpyrazole

    Endogenous Metabolite Others
    4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole (HY-B0876). Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase.
  • HY-122591
    PTUPB

    COX Cancer Metabolic Disease
    PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC50 of 0.9 nM and 1.26 μM, respectively.
  • 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-107337S
    Delapril-d3 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Delapril-d3 hydrochloride is the deuterium labeled Delapril hydrochloride. Delapril hydrochloride is an angiotensin-converting enzyme (ACE) inhibitor for the treatment of cardiovascular diseases.
  • HY-18206A
    Lisinopril dihydrate

    MK-521 dihydrate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Lisinopri dihydrate (MK-521 dihydrate) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
  • HY-10825
    DG051

    Aminopeptidase Metabolic Disease
    DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC50=47 nM.
  • HY-B0279S
    Ramipril-d5

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Ramipril-d5 is the deuterium labeled Ramipril. Ramipril (HOE-498) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.
  • HY-B0231BS
    Enalaprilat-d5 sodium

    MK-422-d5 sodium

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalaprilat (MK-422) D5 Sodium Salt is the deuterium labeled Enalaprilat(MK-422), which is an angiotensin-converting enzyme (ACE) inhibitor.
  • HY-101790A
    ZM223 hydrochloride

    NEDD8-activating Enzyme Cancer
    ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
  • 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-148190
    Sheng Gelieting

    CGT-8012

    Dipeptidyl Peptidase Endocrinology
    Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete.
  • HY-10484
    Pevonedistat hydrochloride

    MLN4924 hydrochloride

    NEDD8-activating Enzyme Cancer
    Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM.
  • HY-125826
    Heptasaccharide Glc4Xyl3

    Others Metabolic Disease
    Heptasaccharide Glc4Xyl3, a covalent inhibitor of endo-xyloglucanases, is used for the identification and analysis of diverse xyloglucan-active enzymes in nature[1].
  • HY-114161
    H-Val-Pro-Pro-OH

    Angiotensin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.
  • HY-136211
    Cystathionine-γ-lyase-IN-1

    Others Metabolic Disease Inflammation/Immunology
    Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC50 of 6.3 μM.
  • HY-18030
    CEP-28122

    Anaplastic lymphoma kinase (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
    Pevonedistat

    MLN4924

    NEDD8-activating Enzyme Cancer
    Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM.
  • HY-B0882S
    Edrophonium-d5 chloride

    Cholinesterase (ChE) Neurological Disease
    Edrophonium-d5 chloride is the deuterium labeled Edrophonium chloride. 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-132337S
    Galanthamine N-Oxide-d3

    Cholinesterase (ChE) Neurological Disease
    Galanthamine N-Oxide-d3 is the deuterium labeled Galanthamine N-Oxide. 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-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-B0744B
    Eflornithine hydrochloride hydrate

    DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate

    Parasite 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
    Tricarballylic acid

    Mitochondrial Metabolism Endogenous Metabolite Inflammation/Immunology
    Tricarballylic acid, a conjugate acid of a tricarballylate, is a competitive inhibitor of the enzyme aconitate hydratase (aconitase; EC 4.2.1.3) with a Ki value of 0.52 mM.
  • HY-109592
    Imidaprilate

    6366A; Imidaprilat

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
  • HY-B0263S1
    Thiabendazole-13C6

    2-(4-Thiazolyl)benzimidazole-13C6

    Mitochondrial Metabolism Parasite Infection
    Thiabendazole-13C6 is the 13C6 labeled Thiabendazole. Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
  • HY-B0231AS
    Enalaprilat D5

    MK-422 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalaprilat D5 (MK-422 D5) is the deuterium labeled Enalaprilat(MK-422), which is an angiotensin-converting enzyme (ACE) inhibitor.
  • HY-145705
    Pencitabine

    DNA/RNA Synthesis Cancer
    Pencitabine (Pen) is an orally active anticancer agent. Pencitabine interferes with DNA synthesis and function by inhibiting multiple nucleotide-metabolizing enzymes and by misincorporation into DNA.
  • HY-114161A
    H-Val-Pro-Pro-OH TFA

    Angiotensin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    H-Val-Pro-Pro-OH (TFA), a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.
  • HY-N2165
    Vicenin 2

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium.
  • HY-N4090
    Vicenin 3

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Vicenin 3 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=46.91 μM) from the aerial parts of Desmodium styracifolium.
  • 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-147388
    hiCE inhibitor-1

    Others Metabolic Disease
    hiCE inhibitor-1, a sulfonamide derivative, is a selective human intestinal enzyme (hiCE) inhibitor with a Ki value of 53.3 nM. hiCE inhibitor-1 can be used to improve Irinotecan (HY-16562)-induced diarrhoea.
  • HY-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, insecticidal, and anti-fungal activities.
  • 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-B0242S2
    Sulfanilamide-d4 hydrochloride

    Sulphanilamide-d4 hydrochloride

    Bacterial Antibiotic Infection
    Sulfanilamide-d4 (Sulphanilamide-d4) hydrochloride is the deuterium labeled Sulfanilamide hydrochloride. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
  • 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-132886
    SARS-CoV-2-IN-6

    SARS-CoV Infection
    SARS-CoV-2-IN-6 is a SARS-CoV-2 3CLpro inhibitor that shows the most potent enzyme inhibitory IC50 value of 73 nM.
  • HY-117281
    Moexipril

    Angiotensin-converting Enzyme (ACE) Apoptosis Neurological Disease Cardiovascular Disease
    Moexipril is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril exhibits antihypertensive and neuroprotective effects -.
  • 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-15345A
    Tetrahydrouridine

    THU; NSC-112907

    Others Cancer
    Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
  • HY-111421
    ODM-204

    Androgen Receptor Cytochrome P450 Cancer
    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
  • HY-B0242S1
    Sulfanilamide-d4

    Sulphanilamide-d4

    Bacterial Antibiotic Infection
    Sulfanilamide-d4 (Sulphanilamide-d4) is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
  • HY-147361
    LDCA

    Apoptosis Lactate Dehydrogenase Cancer
    LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression.
  • 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-101093
    CA-170

    PD-1/PD-L1 Inflammation/Immunology
    CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes.
  • HY-18205
    RXPA 380

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    RXPA 380 is a C-terminal specific angiotensin-converting enzyme (ACE) inhibitor with a Ki of 3 nM. RXPA 380 inhibits C-domain mutants of human recombinant ACE with an IC50 of 2.5 nM.
  • HY-107352
    Fosfenopril

    Fosinoprilat; Fosinoprilic acid; SQ 27519

    Angiotensin-converting Enzyme (ACE) Toll-like Receptor (TLR) NF-κB TNF Receptor Interleukin Related Inflammation/Immunology Cardiovascular Disease
    Fosfenopril (Fosinoprilat) is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes.
  • HY-118694
    TAPI-0

    TNF Receptor MMP Bacterial Cancer Infection
    TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing.
  • 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-100640
    Roflumilast Impurity E

    Phosphodiesterase (PDE) Inflammation/Immunology
    Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
  • HY-N6739
    Beauvericin

    Acyltransferase Infection Cardiovascular Disease
    Beauvericin is a Fusarium mycotoxin. Beauvericin inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 3 μM in an enzyme assay using rat liver microsomes.
  • HY-145326
    Antibacterial agent 67

    Fungal Others
    Antibacterial agent 67 (IC50 = 0.03 μM) has a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 μM).
  • HY-13283
    MF63

    PGE synthase Inflammation/Immunology
    MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively.
  • HY-B1368
    Fenclonine

    4-Chloro-DL-phenylalanine; PCPA; CP-10188

    Tryptophan Hydroxylase Cancer Neurological Disease
    Fenclonine is a selective and irreversible tryptophan hydroxylase inhibitor, which is a rate-limiting enzyme in the biosynthesis of serotonin. Fenclonine can be used in carcinoid syndrome research.
  • 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-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-145197
    MPO-IN-3

    Glutathione Peroxidase Cardiovascular Disease
    MPO-IN-3 is a potent myeloperoxidase (MPO) inhibitor (WO2013068875A1, example 191). Myeloperoxidase (MPO) is a heme-containing enzyme belonging to the peroxidase superfamily.
  • HY-112734
    4'-Methylchrysoeriol

    Cytochrome P450 Cancer
    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
  • HY-N6702
    Enniatin A

    Acyltransferase Infection Cardiovascular Disease
    Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes.
  • HY-146248
    TFMU-ADPr

    Poly(ADP-ribose) Glycohydrolase (PARG) Others
    TFMU-ADPr is a general substrate for monitoring poly(ADP-ribose) glycohydrolase (PARG) activity. TFMU-ADPr can directly report on total PAR hydrolase activity via release of a fluorophore. TFMU-ADPr has excellent reactivity, generality, stability, and usability. TFMU-ADPr is a versatile tool for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.
  • HY-18054
    BVT 2733

    11β-HSD 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-A0116A
    Trandolaprilate hydrate

    Trandolaprilat hydrate; RU 44403 hydrate

    Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Trandolaprilate hydrate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate hydrate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity.
  • HY-A0116
    Trandolaprilate

    Trandolaprilat; RU 44403

    Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Trandolaprilate is a potent angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilate partially inhibits angiotensin-I-mediated c-fos induction. Trandolaprilate is main bioactive metabolite of Trandolapril. Trandolaprilate shows high lipophilicity.
  • HY-130569
    7-Hydroxymethotrexate

    Drug Metabolite Cancer Inflammation/Immunology
    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.
  • 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-118660
    Anhydrotetracycline hydrochloride

    Antibiotic Bacterial Infection
    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.
  • HY-N0529
    Rosmarinic acid

    Labiatenic acid

    Monoamine Oxidase COMT Apoptosis Endogenous Metabolite Cancer
    Rosmarinic acid is a widespread phenolic ester compound in the plants. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.
  • HY-N10361
    Drupanin

    Others Cancer
    Drupanin is a compound isolated from green propolis. Drupanin can selectively inhibit the AKR1C3 enzyme. Drupanin has the potential for the research of breast cancer.
  • HY-B1189
    Meglutol

    Dicrotalic acid; 3-Hydroxy-3-methylglutaric acid

    HMG-CoA Reductase (HMGCR) Autophagy Endogenous Metabolite Cardiovascular Disease
    Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
  • HY-N0125S
    Diosmetin-d3

    Cytochrome P450 Cancer
    Diosmetin-d3 is the deuterium labeled Diosmetin. Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
  • 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-150702
    MAGLi 432

    MAGL Inflammation/Immunology Neurological Disease
    MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
  • HY-76200S
    Voriconazole-d3

    UK-109496-d3

    Fungal Infection
    Voriconazole-d3 (UK-109496-d3) is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • 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-33549
    α-Methyl-p-tyrosine

    Others Cancer
    α-Methyl-p-tyrosine is a competitive inhibitor of the enzyme tyrosine hydroxylase, which converts tyrosine to Levodopa (DOPA). α-Methyl-p-tyrosine is an orally active inhibitor of catecholamine synthesis which inhibits the hydroxylation of tyrosine to DOPA.
  • 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 Parasite 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-144681
    LY3372689

    Tau Protein Neurological Disease
    LY3372689 (Formulaic Ia) is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.
  • HY-W028047
    JFD01307SC

    Bacterial Infection Inflammation/Immunology
    JFD01307SC is a glutamine synthetase inhibitor and anti-tuberculosis agent. JFD01307SC acts as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis.
  • HY-B0378A
    Moexipril hydrochloride

    RS-10085

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects -.
  • 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-146248A
    TFMU-ADPr ammonium

    Poly(ADP-ribose) Glycohydrolase (PARG) Others
    TFMU-ADPr ammonium is a general substrate for monitoring poly(ADP-ribose) glycohydrolase (PARG) activity. TFMU-ADPr ammonium can directly report on total PAR hydrolase activity via release of a fluorophore. TFMU-ADPr ammonium has excellent reactivity, generality, stability, and usability. TFMU-ADPr ammonium is a versatile tool for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.
  • HY-148044
    UNC10201652

    Bacterial Infection
    UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide (HY-126373) processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.
  • 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-117878
    ML345

    Others Metabolic Disease
    ML345 is a potent and selective insulin-degrading enzyme (IDE) small-molecule inhibitor, with an IC50 value of 188 nM. ML345 can be for use as a pharmacophore for drug development in diabetes research.
  • HY-112157
    PF-06751979

    Beta-secretase Neurological Disease
    PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
  • HY-W009993
    3,4-Methylenedioxycinnamic acid

    Others Others
    3,4-Methylenedioxycinnamic acid is an inhibitor of the phenylpropanoid enzyme 4-hydroxycinnamoyl-CoA ligase. 3,4-Methylenedioxycinnamic acid increases the formation of soluble phenolics in particular of vanillic acid.
  • 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
    LY-2584702 tosylate salt

    Ribosomal S6 Kinase (RSK) Cancer
    LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  • HY-144739
    BACE1-IN-8

    Beta-secretase Neurological Disease
    BACE1-IN-8 (compound 70b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 3.9 µM.
  • HY-100283
    CGS 15435

    Others Inflammation/Immunology Endocrinology
    CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.
  • HY-12493B
    LY-2584702 hydrochloride

    Ribosomal S6 Kinase (RSK) Cancer
    LY-2584702 hydrochloride is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  • HY-145302
    Mycobactin-IN-2

    Bacterial Infection
    Mycobactin-IN-2 (compound 49) is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-2 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway.
  • HY-144741
    BACE1-IN-9

    Beta-secretase Neurological Disease
    BACE1-IN-9 (compound 82b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 1.2 µM.
  • HY-B2158
    Chlorotrianisene

    Estrogen Receptor/ERR COX Endocrinology Cardiovascular Disease
    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
  • 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 endocannabinoid-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-114424A
    H-Ile-Pro-Pro-OH hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    H-Ile-Pro-Pro-OH hydrochloride, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.
  • HY-B0384
    Temocapril hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Temocapril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
  • HY-100713
    Temocapril

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Temocapril is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
  • HY-121460
    Spiraprilat

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Spiraprilat is a potent angiotensin-converting enzyme (ACE) inhibitor. Spiraprilat has ability to improve left ventricular (LV) function and metabolism in anesthetized open-chest dogs with acute ventricular failure (ALVF).
  • HY-A0043S
    Cilazapril-d5

    Ro 31-2848-d5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Cilazapril-d5 (Ro 31-2848-d5) is the deuterium labeled Cilazapril. Cilazapril is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.
  • HY-122832
    ABC99

    Wnt Cancer
    ABC99 is an N-hydroxyhydantoin (NHH) carbamate that selectively inhibits the Wnt-deacylating enzyme NOTUM (IC50=13 nM). ABC99 preserves Wnt3A signaling in the presence of NOTUM.
  • HY-114424
    H-Ile-Pro-Pro-OH

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    H-Ile-Pro-Pro-OH, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.
  • 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

    Acetolactate Synthase (ALS) 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-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-127026A
    Quinaprilat hydrate

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator.
  • HY-13635S
    Finasteride-d9

    MK-906-d9

    5 alpha Reductase Cancer
    Finasteride-d9 is deuterium labeled Finasteride. 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-B0592S
    Trandolapril D5

    RU44570 D5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolapril D5 (RU44570 D5) is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF).
  • 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
    LY-2584702 free base

    Ribosomal S6 Kinase (RSK) Cancer
    LY-2584702 free base is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.
  • 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
    Enasidenib

    AG-221

    Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively.
  • HY-112942A
    CMP-Sialic acid sodium salt

    CMP-Neu5Ac sodium salt

    Others Endogenous Metabolite 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-12904
    TCA1

    Bacterial Infection
    TCA1 is a small molecule with activity against drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW.
  • HY-109592S
    Imidaprilate-d5

    6366A-d5; Imidaprilat-d5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Imidaprilate-d5 is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
  • HY-16106
    Talazoparib

    BMN-673; LT-673

    PARP Cancer
    Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.
  • 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-100817
    Rbin-2

    Phosphatase Others
    Rbin-2 is a potent, reversible and selective inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family. Rbin-2 inhibits eukaryotic ribosome biogenesis and is a powerful probe for the eukaryotic ribosome assembly.
  • HY-14530
    Pelitrexol

    AG 2037

    Antifolate Cancer
    Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice.
  • HY-113342
    7-Ketocholesterol

    Endogenous Metabolite Metabolic Disease
    7-Ketocholesterol, toxic oxysterol, inhibits the rate-limiting step in bile acid biosynthesis cholesterol 7 alpha-hydroxylase, as well as strongly inhibiting HMG-CoA reductase (the rate-limiting enzyme in cholesterol biosynthesis). 7-Ketocholesterol induces cell apoptosis.
  • HY-127026
    Quinaprilat

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinaprilat is an orally active non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat acts as anti-hypertensive agent and vasodilator.
  • 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-145301
    Mycobactin-IN-1

    Bacterial Infection
    Mycobactin-IN-1 (compound 44), a pyrazoline analogue, is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway.
  • HY-117281S
    Moexipril-d5

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Moexipril-d5 is the deuterium labeled Moexipril. Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure.
  • HY-P0318
    Hemorphin-7

    Opioid Receptor Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
  • HY-18062S
    Pyrimethamine-d3

    Antifolate Parasite Infection
    Pyrimethamine-d3 (Pirimecidan-d3) is the deuterium labeled Pyrimethamine. Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).
  • 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

    Thrombin Factor Xa 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-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 and KPC) and class C (AmpC) enzymes. Relebactam shows antibacterial activity.
  • HY-D0843S
    N-Ethylmaleimide-d5

    NEM-d5

    Cathepsin Deubiquitinase Others
    N-Ethylmaleimide-d5 (NEM-d5) is the deuterium labeled N-Ethylmaleimide. 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-14768
    Favipiravir

    T-705

    DNA/RNA Synthesis Influenza Virus SARS-CoV Bacterial 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 Bacterial 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-14519D
    Methotrexate monohydrate

    Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate

    Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis Bacterial Cancer Inflammation/Immunology
    Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, 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-106406
    Benzylacyclouridine

    BAU; 5-Benzylacyclouridine

    Others Cancer
    Benzylacyclouridine (BAU) is a potent and specific inhibitor of uridine phosphorylase, the first enzyme in the catabolism of uridine. Benzylacyclouridine can modulate the cytotoxic side effects of 5-fluorouracil (5-FU) and its derivatives.
  • 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 (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
  • HY-112205
    RR-11a

    Others Cancer
    RR-11a is a synthetic enzyme inhibitor of Legumain (IC50=31-55 nM). RR-11a can be used for the research of cancer and acute myocardial infarction (AMI).
  • HY-A0115
    Ramiprilat

    HOE 498 diacid; Ramipril diacid

    Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research.
  • HY-113829S
    Valnemulin-d6 TFA

    Bacterial Antibiotic Infection
    Valnemulin-d6 TFA is the deuterium labeled Valnemulin TFA. Valnemulin TFA is a pleuromutilin antibiotic which inhibits protein synthesis in bacteria by binding the peptidyl transferase enzyme in the 50s ribosomal subunit.
  • HY-B1451S
    Imidapril-d3 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Imidapril-d3 hydrochloride (TA-6366-d3) is the deuterium labeled Imidapril hydrochloride. Imidapril hydrochloride (TA-6366) is the hydrochloride salt of Imidapril, an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.
  • HY-W032848
    Tinoridine

    Y-3642

    COX Inflammation/Immunology
    Tinoridine (Y-3642) is an orally active non-steroidal anti-inflammatory agent with potent antiperoxidative ability and radical scavenger activity. Tinoridine acts function by inhibiting COX enzyme, involves in hepatotoxicity inhibition. .
  • HY-103056
    DDD85646

    DNA/RNA Synthesis Parasite Infection
    DDD85646 is a potent inhibitor of trypanosoma brucei N-myristoyltransferase (TbNMT IC50=2 nm; hNMTIC50=4 nm). The enzyme N-myristoyltransferase (NMT) is a potential drug target for human African trypanosomiasis.
  • HY-144465
    IDO1-IN-15

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    IDO1-IN-15 is a potent IDO1 inhibitor (IC50=127 nM). IDO1-IN-15 has comparable potency against IDO1 enzyme in vitro with Epacadostat.
  • HY-12219
    MSI-1436

    Trodusquemine; Aminosterol-1436

    Phosphatase Endocrinology
    MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
  • HY-145954
    NAT2-IN-1

    APA

    Others Cancer
    NAT2-IN-1 (APA) is an inhibitor of drug metabolic enzyme N-acetyltransferase 2 (NAT2). NAT2-IN-1 can selectively kill slow NAT2 cells.
  • HY-129035
    PFI-653

    Vanin-1-IN-1

    Others Metabolic Disease Inflammation/Immunology
    PFI-653 (Vanin-1-IN-1) is an inhibitor of vanin-1 enzyme which is a cell surface associated, giycosyiphosphatidyS inositol (GPi) anchored protein and plays an important role in metabolism and inflammation.
  • 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-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-144371
    DHODH-IN-20

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer Inflammation/Immunology
    DHODH-IN-20 (Compound 133) is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-20 inhibits tumor growth. DHODH-IN-20 has the potential for the research of acute myelogenous leukemia.
  • 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-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-B0477AS1
    Quinapril-d5 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Quinapril-d5 hydrochloride (CI-906-d5) is the deuterium labeled Quinapril hydrochloride. Quinapril hydrochloride (CI-906) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications.
  • HY-B0690
    Fosinopril

    SQ28555 free acid

    Angiotensin-converting Enzyme (ACE) Apoptosis Cardiovascular Disease
    Fosinopril (SQ28555 free acid) is the ester prodrug of angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.18 μM. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with an Ki value of 1.675 μM.
  • HY-101930
    BMS-816336

    11β-HSD 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-109000A
    Afabicin disodium

    Debio 1450 disodium; AFN-1720 disodium

    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-138843
    FTO-IN-1

    Fat Mass and Obesity-associated Protein (FTO) Cancer Metabolic Disease
    FTO-IN-1 is a fat mass and obesity-associated enzyme (FTO) inhibitor extracted from patent WO2018157843A1, compound 32, with an IC50 of <1 μM. FTO-IN-1 can be used for the research of cancer.
  • HY-18206S
    Lisinopril-d5

    MK-521-d5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Lisinopril-d5 (MK-521-d5) is the deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
  • 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-141412
    D-(-)-3-Phosphoglyceric acid disodium

    3-Phospho-D-glyceric acid disodium

    Enolase Infection
    D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalysed process of glycolysis. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase.
  • HY-14519A
    Methotrexate disodium

    Amethopterin disodium; CL14377 disodium; WR19039 disodium

    Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis Bacterial 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-N0214A
    Peimisine hydrochloride

    Ebeiensine hydrochloride

    mAChR Angiotensin-converting Enzyme (ACE) Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research.
  • HY-B0231A
    Enalaprilat

    MK-422 anhydrous

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalaprilat (MK-422 anhydrous), the active metabolite of the oral prodrug Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat can be used for the research of hypertension.
  • 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-100713S
    Temocapril-d5

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Temocapril-d5 is the deuterium labeled Temocapril. Temocapril is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
  • 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-N0214
    Peimisine

    Ebeiensine

    mAChR Angiotensin-converting Enzyme (ACE) Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research.
  • HY-116301
    CAY10502

    Phospholipase Inflammation/Immunology
    CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases.
  • HY-138830
    TAK-418

    Histone Demethylase Neurological Disease
    TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models.
  • 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-115537
    NAE-IN-M22

    Apoptosis Cancer
    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-B1320
    Meclofenamic acid sodium

    Meclofenamate sodium

    Gap Junction Protein Endogenous Metabolite Inflammation/Immunology
    Meclofenamic acid (Meclofenamate) 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-B2158S
    Chlorotrianisene-d9

    Estrogen Receptor/ERR COX Endocrinology Cardiovascular Disease
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
  • HY-111383
    LX2343

    Beta-secretase PI3K Amyloid-β Autophagy Neurological Disease
    LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of clearance.
  • HY-138843A
    FTO-IN-1 TFA

    Fat Mass and Obesity-associated Protein (FTO) Cancer Metabolic Disease
    FTO-IN-1 TFA is a fat mass and obesity-associated enzyme (FTO) inhibitor extracted from patent WO2018157843A1, compound 32, with an IC50 of <1 μM. FTO-IN-1 TFA can be used for the research of cancer.
  • HY-B0382S
    Fosinopril-d5 sodium

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Fosinopril-d5 sodium (SQ28555-d5 sodium) is the deuterium labeled Fosinopril sodium. Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
  • 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

    Captopril bromo analog

    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; 3-Mercapto-2-methylpropionic 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-144798
    FWM-5

    SARS-CoV Infection
    FWM-5 is a potent NSP13 helicase inhibitor. SARS-COV-2 NSP13 helicase enzyme plays crucial role in the virus life cycle. FWM-5 has the potential for the research of infection diseases.
  • HY-N0356S
    (+/-)-Catechin Gallate-13C3

    COX Cancer
    (+/-)-Catechin Gallate-13C3 is the 13C-labeled (-)-Catechin gallate. (-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of COX-1 and COX-2 enzymes.
  • HY-B0231
    Enalaprilat dihydrate

    MK-422

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Enalaprilat dihydrate (MK-422), the active metabolite of the oral prodrug Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat dihydrate can be used for the research of hypertension.
  • HY-100877
    GCN2-IN-1

    A-92

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-1 (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
  • HY-137772
    Captopril EP Impurity E

    Isobutyrylproline

    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
    Polygalaxanthone III

    Cytochrome P450 Inflammation/Immunology
    Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
  • HY-151806
    HadAB-IN-1

    Bacterial Infection Inflammation/Immunology
    HadAB-IN-1 is a potent HadAB inhibitor. HadAB-IN-1 inhibits HadAB enzyme complexes activity with an IC50 value of 0.03 μM. HadAB-IN-1 also affects mycolic acid biosynthesis in Mycobacterium tuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB).
  • HY-130569S
    7-Hydroxymethotrexate-d3 sodium

    Drug Metabolite Cancer Inflammation/Immunology
    7-Hydroxymethotrexate-d3 (sodium) is deuterium labeled 7-Hydroxymethotrexate. 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.
  • 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-145272
    ELOVL1-IN-3

    Others Neurological Disease
    ELOVL1-IN-3 (Compound 22) is a potent and orally active inhibitor of elongation of very long chain fatty acid 1 (ELOVL1) enzyme. ELOVL1-IN-3 serves as a useful tool for researching adrenoleukodystrophy (ALD)[1].
  • HY-19414
    MLN-4760

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).
  • 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-142924
    ATR-IN-8

    ATM/ATR Cancer
    ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombination repair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3).
  • HY-B0592A
    Trandolapril hydrochloride

    RU44570 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Trandolapril (RU44570) hydrochloride is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolapril hydrochlorideat. Trandolapril hydrochloride is an orally active 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-137954
    GRL-0496

    SARS-CoV Infection
    GRL-0496 is a potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitor, with an IC50 of 30 nM in both enzyme inhibitory and antiviral assays. GRL-0496 shows SARS-CoV antiviral activity, with an EC50 of 6.9 μM.
  • 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-16677A
    Mofegiline hydrochloride

    MDL72974A

    Monoamine Oxidase Neurological Disease
    Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO).
  • 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

    Adrenergic Receptor 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-129239
    Farudodstat

    ASLAN003

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Apoptosis Cancer
    Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
  • HY-144169
    DHODH-IN-19

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer Inflammation/Immunology
    DHODH-IN-19 is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-19 inhibits tumor growth. DHODH-IN-19 has the potential for the research of cancer and inflammation disease (extracted from patent WO2021238881A1, compound 1).
  • HY-148001
    EWP 815

    Phosphatase Dopamine β-hydroxylase Others
    EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity.
  • HY-101494
    Temuterkib

    LY3214996

    ERK Cancer
    Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
  • HY-130794
    ALK/ROS1-IN-1

    Anaplastic lymphoma kinase (ALK) ROS Kinase 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-10679A
    PF-03049423

    Phosphodiesterase (PDE) Neurological Disease
    PF-03049423 (Compound PF-5) is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 can be used for the research of acute ischaemic stroke.
  • HY-110217
    BMS-566419

    Others Others
    BMS-566419 is an acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase (IMPDH). Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme in the de novo synthesis of guanosine nucleotides. BMS-566419 has clinical utility for the research of transplant rejection.
  • HY-W021879
    DSRM-3716

    5-Iodoisoquinoline

    Others Neurological Disease
    DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. DSRM-3716 is selective against other NAD +-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection.
  • HY-33298
    LM10

    Others Cancer
    LM10 is a potent inhibitor of tryptophan 2,3-dioxygenase (TDO). Tryptophan 2,3-dioxygenase (TDO) is an unrelated hepatic enzyme that also degrades tryptophan along the kynurenine pathway. LM10 has the potential for the research of cancer diseases.
  • 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-B0876A
    Fomepizole hydrochloride

    4-Methylpyrazole hydrochloride

    Cytochrome P450 Metabolic Disease
    Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning.
  • HY-147691
    MPO-IN-5

    Glutathione Peroxidase Potassium Channel Inflammation/Immunology
    MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1.
  • HY-10237
    Boceprevir

    EBP 520; SCH 503034

    HCV Protease HCV SARS-CoV 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. Boceprevir inhibits SARS-CoV-2 3CL pro activity.
  • 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-108681
    680C91

    Others Cancer Inflammation/Immunology Neurological Disease
    680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a Ki of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease.
  • 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

    Acetyl-CoA Carboxylase 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-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial 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. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
  • HY-143582
    ATX inhibitor 9

    Others Cancer
    ATX inhibitor 9 is a potent inhibitor of ATX. ATX inhibitor 9 is a thickened heteroaryl derivatives compound. Autotaxin (ATX), also known as ENPP2, is a secreted enzyme that is highly expressed mainly in cancer cells, bronchial epithelial cells and alveolar macrophages in the lung. ATX inhibitor 9 has the potential for the research of cancer or fibrous degenerative disease (extracted from patent WO2021078227A1, compound 3).
  • HY-A0115S1
    Ramiprilat-d5

    Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Cardiovascular Disease
    Ramiprilat-d5 is deuterium labeled Ramiprilat. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research.
  • 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-119402
    TP-021

    BCL6-IN-8c

    Bcl-2 Family Cancer
    TP-021 (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-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-120019
    Ac-YVAD-CHO

    L-709049

    Interleukin Related Inflammation/Immunology
    Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO can suppress the production of mature IL-lβ.
  • HY-W017464
    NAPQI

    Endogenous Metabolite Metabolic Disease
    NAPQI is the toxic metabolite of Acetaminophen (HY-66005). NAPQI is also an inhibitor of enzymes in the vitamin K cycle. NAPQI is rapidly detoxified by glutathione (GSH), but in situations of GSH deficiency, excess NAPQI reacts with cysteine residues in proteins, causing cell death and toxicity in the liver.
  • HY-16990
    Ac-YVAD-cmk

    Caspase-1 Inhibitor II

    Caspase Inflammation/Immunology
    Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases.
  • HY-125986
    GK187

    Phospholipase Neurological Disease
    GK187 is a potent and selective Group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor with an XI(50) value of 0.0001. GK187 can be used for researching various neurological disorders.
    [The XI(50) is the mole fraction of the inhibitor in the total substrate interface required to inhibit the enzyme by 50%.]
  • HY-148396
    UCK2 Inhibitor-3

    DNA/RNA Synthesis Cancer Infection
    UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM.
  • HY-107761
    JMV 390-1

    Others Neurological Disease
    JMV 390-1 (Compound 6a) is a potent multipeptidase inhibitor. JMV 390-1 behaves as a full inhibitor of the major neurotensin (NT)/neuromedin N (NN) degrading enzymes in vitro with IC50 values from 30 to 60 nM. JMV 390-1 increases endogenous recovery of NT and NN from slices of mice hypothalamus depolarized with potassium.
  • 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-A0166S
    Cilastatin-15N,d3

    MK0791-15N,d3

    Bacterial Antibiotic Infection
    Cilastatin-15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. 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-N2533
    Cyanidin 3-sambubioside chloride

    Cyanidin-3-O-sambubioside chloride

    Influenza Virus Angiotensin-converting Enzyme (ACE) Cancer Infection Inflammation/Immunology
    Cyanidin 3-sambubioside chloride (Cyanidin-3-O-sambubioside chloride), a major anthocyanin, a natural colorant, and is a potent NO inhibitor. Cyanidin 3-sambubioside chloride is a H274Y mutation inhibitor, and inhibits influenza neuraminidase activity with an IC50 of 72 μM. Cyanidin 3-sambubioside chloride inhibits angiotensin-converting enzyme (ACE) activity and has antioxidant, anti-angiogenic and antiviral properties.
  • 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-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-111458
    GSK2643943A

    Deubiquitinase Cancer
    GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
  • 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
    Enniatin B

    Acyltransferase ERK Cancer Infection Cardiovascular Disease
    Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes. Enniatins B decreases the activation of ERK (p44/p42).
  • 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-110159
    (E/Z)-Teriflunomide

    (E/Z)-A77 1726

    Dihydroorotate Dehydrogenase Infection Inflammation/Immunology
    (E/Z)-Teriflunomide ((E/Z)-A77 1726) is the active metabolite of Leflunomide (HY-B0083). Leflunomide is an immunomodulatory agent that may exert effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). Leflunomide can be used for the research of rheumatoid arthritis (RA).
  • HY-114782
    H-Tyr-Tyr-OH

    L-Tyrosyl-L-tyrosine

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    H-Tyr-Tyr-OH (L-Tyrosyl-L-tyrosine) is an antihypertensive peptide. H-Tyr-Tyr-OH inhibits angiotensin I-converting enzyme (ACE) with an IC50 value of 0.028 mg/mL. H-Tyr-Tyr-OH can be used for the research of high blood pressure.
  • HY-100313A
    YM-53601

    Farnesyl Transferase HCV Infection Metabolic Disease
    YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.
  • 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
    2,4-Diamino-6-hydroxypyrimidine

    NO Synthase Inflammation/Immunology
    2,4-Diamino-6-hydroxypyrimidine is a specific GTP cyclohydrolase I inhibitor (the rate-limiting enzyme in de novo pterin synthesis). 2,4-Diamino-6-hydroxypyrimidine blocks Tetrahydrobiopterin (BH4) synthesis and suppresses NO production.
  • 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-10679
    PF-03049423 free base

    Phosphodiesterase (PDE) Neurological Disease
    PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke.
  • HY-P0266B
    N-Acetyl-Ser-Asp-Lys-Pro acetate

    Ac-SDKP acetate

    Angiotensin-converting Enzyme (ACE) Inflammation/Immunology
    N-Acetyl-Ser-Asp-Lys-Pro (Ac-SDKP) acetate is a specific substrate for the N-terminal active site of angiotensin-converting enzyme (ACE). N-Acetyl-Ser-Asp-Lys-Pro acetate is a natural inhibitor of pluripotent hematopoietic stem cell proliferation. Anti-inflammatory and antifibrotic properties.
  • 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-W012159
    Methionylserine

    H-MET-SER-OH

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Methionylserine (H-MET-SER-OH) is a methionine- and serine-containing dipeptide. Methionylserine binds to and translocation via intestinal di/tri-peptide transporter 1 (hPEPT1) with a Km value of 0.2 mM. Methionylserine inhibits ACE enzyme activity. Methionylserine can be used in the research of hypension.
  • HY-130517
    Cdc7-IN-5

    CDK Cancer
    Cdc7-IN-5 (compound I-B) 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-141622
    SDZ 224-015

    Interleukin Related Caspase SARS-CoV Infection Inflammation/Immunology
    SDZ 224-015 is an orally active inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1. SDZ 224-015 possesses anti-COVID-19 activity, targeting M pro (IC50 of 30 nM).
  • HY-N7450
    Icariside D2

    Angiotensin-converting Enzyme (ACE) Apoptosis HIV Cancer Infection Inflammation/Immunology
    Icariside D2, isolated from Annona glabra fruit, inhibits angiotensin-converting enzyme. Icariside D2 shows significant cytotoxic activity on the HL-60 cell line with the IC50 value of 9.0 ± 1.0 μM. Icariside D2 induces apoptosis .
  • 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-111558
    Bobcat339

    DNA Methyltransferase Cancer
    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-145831
    sEH/AChE-IN-1

    Cholinesterase (ChE) Inflammation/Immunology Neurological Disease
    sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD).
  • HY-19676
    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.
  • HY-130244
    BACE1-IN-5

    Beta-secretase Neurological Disease
    BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.
  • 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-14519S
    Methotrexate-d3

    Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis Cancer Inflammation/Immunology
    Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. 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-N0279
    Cardamonin

    Cardamomin; Alpinetin chalcone

    NF-κB STAT Wnt β-catenin Bcl-2 Family Apoptosis Cancer Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    Cardamonin can be found from cardamom, and target various signaling molecules, transcriptional factors, cytokines and enzymes. Cardamonin can inhibit mTOR, NF-κB, Akt, STAT3, Wnt/β-catenin and COX-2. Cardamonin shows anticancer, anti-inflammatory, antimicrobial and antidiabetic activities.
  • HY-143432
    Cdc7-IN-18

    CDK Cancer
    Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC50 of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC50 of 53.62 nM in COLO205 cells.
  • HY-115883
    PptT-IN-2

    Others Infection Inflammation/Immunology
    PptT-IN-2 (compound 5k) is a potent inhibitor of with phosphopantetheinyl phosphoryl transferase (PptT) an IC50 of 2.5 μM. Phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. PptT-IN-2 has the potential for the research of tuberculosis.
  • HY-145832
    sEH/AChE-IN-2

    Cholinesterase (ChE) Inflammation/Immunology Neurological Disease
    sEH/AChE-IN-2 (Compound 12b) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-2 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-2 has the potential for the research of Alzheimer's disease (AD).
  • 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-115884
    PptT-IN-3

    Others Infection Inflammation/Immunology
    PptT-IN-3 (compound 5p) is a potent inhibitor of with phosphopantetheinyl phosphoryl transferase (PptT) an IC50 of 3.5 μM. Phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. PptT-IN-3 has the potential for the research of tuberculosis.
  • HY-110197
    6bK

    Others Metabolic Disease
    6bK is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC50 value of 50 nM. 6bK increases circulating insulin in high-fat-fed mice. Acute administration of 6bK enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice.
  • HY-A0230
    Spirapril

    SCH 33844

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Spirapril is a potent and cross the blood-brain barrier 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-115882
    PptT-IN-1

    Others Infection Inflammation/Immunology
    PptT-IN-1 (compound 5j) is a potent inhibitor of with phosphopantetheinyl phosphoryl transferase (PptT) an IC50 of 2.8 μM. Phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacterium tuberculosis. PptT-IN-1 has the potential for the research of tuberculosis.
  • HY-109785A
    (R)-Gyramide A hydrochloride

    Bacterial 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-B0150S
    Nicotinamide-d4

    Niacinamide-d4; Nicotinic acid amide-d4

    Sirtuin Endogenous Metabolite Neurological Disease Cancer
    Nicotinamide-d4 (Niacinamide-d4) is the deuterium labeled Nicotinamide. 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-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-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-70013S
    Abiraterone-D4

    CB-7598-D4

    Cytochrome P450 Cancer
    Abiraterone-D4 (CB-7598-D4) is the deuterium labeled Abiraterone. 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-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-108542
    Tautomycetin

    Phosphatase Antibiotic Inflammation/Immunology
    Tautomycetin is a potent and specifical PP1 inhibitor with the potential apoptosis-inducing activity. Tautomycetin inhibits purified PP1 and PP2A enzymes with IC50s of 1.6 nM and 62 nM, respectively. Tautomycetin is an antifungal antibiotic and has immunosuppressive effects in vivo. Tautomycetin can be used as a novel powerful tool to elucidate the physiological roles of PP1 in various biological events.
  • HY-145953
    VY-3-135

    Others Cancer
    VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.
  • HY-114196
    Aclimostat

    ZGN-1061

    Others Metabolic Disease
    Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells.
  • HY-146171
    FabH-IN-1

    Bacterial Infection
    FabH-IN-1 (compound 3f) is an inhibitor of bacterial 3-oxoacyl-[acyl-carrier-protein] synthase 3 (FabH) enzyme which is a broad-spectrum antimicrobial target. FabH-IN-1 is effective against gram-positive and gram-negative. FabH-IN-1 is also a good antioxidant.
  • HY-112732
    Sparfosic acid

    Apoptosis Cancer Metabolic Disease
    Sparfosic acid, a DNA antimetabolite agent, is a potent inhibitor of aspartate transcarbamoyl transferase, the enzyme catalyzing the second step of de novo pyrimidine biosynthesis. Sparfosic acid synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.
  • 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

    Cytochrome P450 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-B0368A
    Captopril hydrochloride

    SQ 14225 hydrochloride

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Captopril (SQ 14225) hydrochloride, 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 hydrochloride is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM.
  • 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-146699
    MtTMPK-IN-5

    Bacterial Thymidylate Synthase Infection
    MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis.
  • HY-133116
    4-Hydroxyatomoxetine

    Adrenergic Receptor 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-112226
    VRT-043198

    Caspase Drug Metabolite Inflammation/Immunology
    VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits Ki values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively.
  • HY-145381
    11β-HSD1-IN-6

    11β-HSD Metabolic Disease
    11β-HSD1-IN-6 is a an 11β-HSD-1 inhibitor. The 11β hydroxysteroid dehydrogenase enzymes (11β-HSDs) mediate the interconversion of the glucocorticoid (GC) corticosterone or cortisol to an inactive form, 11-dehydrocorticosterone (11-DHC) or Cortisone, respectively.
  • HY-P1435
    NoxA1ds

    NADPH Oxidase Cardiovascular Disease
    NoxA1ds is a highly efficacious and selective Nox1 (NADPH oxidase isoform 1) inhibitor. NoxA1ds establishes a critical interaction site for Nox1-NOXA1 binding required for enzyme activation. NoxA1ds can be used for the research of hypertension, atherosclerosis and neoplasia.
  • HY-B0476S
    Phenacetin-d5

    Acetophenetidin-d5

    COX Inflammation/Immunology
    Phenacetin-d5 (Acetophenetidin-d5) is the deuterium labeled Phenacetin. 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-101930B
    (R)-BMS-816336

    11β-HSD 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-100313
    YM-53601 free base

    Farnesyl Transferase HCV Metabolic Disease
    YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation.
  • HY-15463S2
    Imatinib-d3 hydrochloride

    STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride

    PDGFR SARS-CoV c-Kit Bcr-Abl Autophagy Cancer
    Imatinib-d3 (STI571-d3) hydrochloride is the deuterium labeled Imatinib. 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-116804
    ZLD1039

    Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
  • HY-W015007S
    Metyrosine-13C9,15N,d7

    COX Cardiovascular Disease
    Metyrosine-13C9,15N,d7 is the deuterium, 13C-, and 15-labeled Metyrosine. 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-151802
    CPUL1

    Others Cancer
    CPUL1 is a TrxR inhibitor, which shows proliferation-inhibitory and anti-metastatic activity against A549 cells. CPUL1 influences EMT (epithelial-mesenchymal transition) via inducing ROS-mediated ERK/JNK signaling by inhibiting TrxR1 enzyme activity. CPUL1 in combination with α-Lipoic Acid (HY-N0492) or Dithiodipropionic acid (HY-W014395) is more effective.
  • 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 s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.
  • 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-147261
    B026

    Histone Acetyltransferase Cancer
    B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.
  • HY-B0815S
    Chlorpyrifos-d10

    Cholinesterase (ChE) Neurological Disease
    Chlorpyrifos-d10 is the deuterium labeled Chlorpyrifos. 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-119397
    KDM5-C49

    KDOAM-20

    Histone Demethylase Cancer
    KDM5-C49 (KDOAM-20) is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 can be used for the research of cancer.
  • HY-B1451
    Imidapril hydrochloride

    TA-6366

    Angiotensin-converting Enzyme (ACE) MMP Metabolic Disease Cardiovascular Disease
    Imidapril hydrochloride (TA-6366) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril hydrochloride suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril hydrochloride can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research.
  • HY-147110
    APX2039

    Fungal Infection Inflammation/Immunology
    APX2039 is an orally active and potent inhibitor of the fungal Gwt1 enzyme. APX2039 has extremely potent anticryptococcal activity against C. neoformans and C. gattii. APX2039 blocks the localization of GPI (glycosylphosphatidyl inositol)-anchored cell wall mannoproteins. APX2039 can be used for Cryptococcal meningitis (CM) research.
  • 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-117275S1
    Meclofenamic acid-13C6

    Meclofenamate-13C6

    Gap Junction Protein Endogenous Metabolite Inflammation/Immunology
    Meclofenamic acid-13C6 is the 13C6 labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), 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-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-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-N6798
    Myriocin

    Thermozymocidin; ISP-I

    HCV Antibiotic Infection
    Myriocin (Thermozymocidin), a fungal metabolite could be 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 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-10237S
    Boceprevir-d9

    EBP 520-d9; SCH 503034-d9

    HCV Protease HCV SARS-CoV Infection
    Boceprevir-d9 (EBP 520-d9) is the deuterium labeled Boceprevir. 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. Boceprevir inhibits SARS-CoV-2 3CL pro activity.
  • 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-136490
    Psychosine

    Galactosylsphingosine

    PKC Cancer Neurological Disease
    Psychosine (Galactosylsphingosine), a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell types including, most relevantly to globoid cell leukodystrophy (GLD), oligodendrocytes. Psychosine causes cell death at least in part via apoptosis. Psychosine also is an inhibitor of PKC.
  • 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-145270
    ELOVL1-IN-2

    Others Metabolic Disease
    ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .
  • HY-B0150S2
    Nicotinamide-13C6

    Niacinamide-13C6; Nicotinic acid amide-13C6

    Endogenous Metabolite Sirtuin Neurological Disease Cancer
    Nicotinamide-13C6 (Niacinamide-13C6) is the 13C-labeled Nicotinamide. 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-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-B1451A
    Imidapril

    TA-6366 free base

    Angiotensin-converting Enzyme (ACE) MMP Metabolic Disease Cardiovascular Disease
    Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research.
  • HY-112198
    AZ31

    ATM/ATR Cancer
    AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC50 of <1.2 nM for ATM enzyme, and an IC50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer.
  • 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-108263B
    (R)-3-Hydroxy Midostaurin

    (R)-CGP52421

    FLT3 Drug Metabolite Cancer
    (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).
  • HY-143897
    PIM1-IN-3

    Pim Apoptosis Cancer
    PIM1-IN-3 (Compound HL8) is a potent inhibitor of PIM1. PIM1-IN-3 shows selective inhibition for the PIM-1 enzyme. PIM1-IN-3 induces apoptosis efficiently in Colo320 cells. PIM1-IN-3 has the potential for the research of cancer diseases.
  • HY-17514S
    Itraconazole-d5

    R51211-d5

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. 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-B0368S
    Captopril-d3

    SQ 14225-d3

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Captopril-d3 is deuterium labeled Captopril. 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-117275
    Meclofenamic acid

    Meclofenamate

    Fat Mass and Obesity-associated Protein (FTO) Potassium Channel Gap Junction Protein Endogenous Metabolite Metabolic Disease Inflammation/Immunology Neurological Disease
    Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) 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. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively.
  • HY-117275A
    Meclofenamic acid sodium hydrate

    Meclofenamate sodium hydrate

    Fat Mass and Obesity-associated Protein (FTO) Potassium Channel Gap Junction Protein Endogenous Metabolite Metabolic Disease Inflammation/Immunology Neurological Disease
    Meclofenamic acid (Meclofenamate) sodium hydrate is a non-steroidal anti-inflammatory agent. Meclofenamic acid sodium hydrate is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid sodium hydrate competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid sodium hydrate is a non-selective gap-junction blocker. Meclofenamic acid sodium hydrate inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively.
  • HY-110167
    TFC 007

    PGE synthase Ligands for Target Protein for PROTAC Cancer
    TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).
  • HY-115620
    AQX-016A

    Phosphatase PI3K TNF Receptor Inflammation/Immunology
    AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research.
  • HY-101930A
    (Rac)-BMS-816336

    11β-HSD Metabolic Disease
    (Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of human and mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability.
  • HY-B0760S
    Fenofibric acid-d6

    PPAR COX Metabolic Disease
    Fenofibric acid-d6 (FNF acid-d6) is the deuterium labeled Fenofibric acid. 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-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-144874
    AZ3391

    PARP Cancer Neurological Disease
    AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23).
  • HY-13269
    BMS-707035

    HIV HIV Integrase Infection Inflammation/Immunology
    BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1).
  • 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-B0150S1
    Nicotinamide-15N,13C3

    Niacinamide-15N,13C3; Nicotinic acid amide-15N,13C3

    Endogenous Metabolite Sirtuin Neurological Disease Cancer
    Nicotinamide-15N,13C3 is the 13C-labeled and 15N-labeled Nicotinamide. 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-143898
    PIM1-IN-4

    Pim Cancer
    PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases.
  • HY-P0005
    Glucagon (Human)

    Glukagon; Hyperglycemic-glycogenolytic factor

    Others Metabolic Disease
    Glucagon exhibits marked effects on protein and amino acid metabolism. Glucagon inhibits the incorporation of amino acids into protein of liver, muscle, and pancreas, to increase excretion of nitrogen, to promote hepatic urea synthesis, and to increase the concentration of hepatic transaminases and urea cycle enzymes. Glucagon can promote the hepatic uptake of amino acids, to enhance their incorporation into liver glycogen, and to depress the concentration of amino acids in blood.
  • 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-117275S
    Meclofenamic acid-d4

    Meclofenamate-d4

    Gap Junction Protein Endogenous Metabolite Inflammation/Immunology
    Meclofenamic acid-d4 (Meclofenamate-d4) is the deuterium labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), 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-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-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 with an IC50 of 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-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-108474S
    Nolatrexed-d4 dihydrochloride

    Thymidylate Synthase Cancer
    Nolatrexed-d4 dihydrochloride (AG 337-d4) is the deuterium labeled Nolatrexed dihydrochloride. 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-15259
    CP-640186

    Acetyl-CoA Carboxylase Metabolic Disease
    CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation.
  • HY-146696
    mEH-IN-1

    Epoxide Hydrolase Cancer Neurological Disease Cardiovascular Disease
    mEH-IN-1 (Compound 62) is a potent microsomal epoxide hydrolase (mEH) inhibitor with the IC50 of 2.2 nM. The mEH is a mammalian α/β-fold hydrolase enzyme, expressed in almost all tissues, hydrolyzes a wide range of epoxide containing molecules. The mEH is mainly localized in the endoplasmic reticulum (ER) of eukaryotic cells. mEH-IN-1 can be used for the research of preeclampsia, hypercholanemia and cancer.
  • HY-B0124S
    Zonisamide-d4

    Carbonic Anhydrase Calcium Channel Sodium Channel Neurological Disease
    Zonisamide-d4 (AD 810-d4) is the deuterium labeled Zonisamide. 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-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-15259A
    CP-640186 hydrochloride

    Acetyl-CoA Carboxylase Metabolic Disease
    CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation.
  • 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-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-13560
    AVN-944

    VX-944

    Arenavirus DNA/RNA Synthesis Apoptosis Caspase Bcl-2 Family Cancer Infection
    AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.
  • 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

    AAK1 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-125604
    WCK-4234

    Bacterial Infection
    WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibits class A, C, and D β-lactamases activity. WCK-4234 lacks direct antibacterial activity. WCK-4234 potentiates imipenem and meropenem against Enterobacteriaceae with OXA-48/OXA-181 or KPC enzymes, or with combinations of impermeability and AmpC or ESBL activity. WCK-4234 distinctively overcomes resistance mediated by OXA-type carbapenemases.
  • 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-15275
    BMS-265246

    CDK Angiotensin-converting Enzyme (ACE) Cancer Infection
    BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.
  • HY-120179
    LP-922761

    AAK1 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-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-142944
    DNA-PK-IN-2

    DNA-PK Cancer
    DNA-PK-IN-2 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-2 has the potential for the research of cancer diseases (extracted from patent WO2021136462A1, compound 1).
  • HY-126003
    ALDH1A1-IN-2

    Aldehyde Dehydrogenase (ALDH) Cancer
    ALDH1A1-IN-2 is a potent inhibitor of aldehyde dehydrogenase 1a1 (aldh1a1). Aldehyde dehydrogenases (ALDH) constitute a family of enzymes that play a critical role in oxidizing various cytotoxic xenogenic and biogenic aldehydes. ALDH1A1-IN-2 has the potential for the research of cancer, inflammation, or obesity (extracted from patent WO2019089626A1, compound 295).
  • 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-142943
    DNA-PK-IN-1

    DNA-PK Cancer
    DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1).
  • HY-146675
    COX/5-LOX-IN-1

    COX Inflammation/Immunology
    COX/5-LOX-IN-1 (compound 6b) is a potent and dual inhibitor of COX/5-LOX with IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively. COX/5-LOX-IN-1 has the potential for the research of inflammation diseases.
  • 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-141431
    Cbl-b-IN-2

    E3 Ligase Ligand-Linker Conjugates Cancer Inflammation/Immunology
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
  • 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-144770
    SARS-CoV-2-IN-13

    SARS-CoV Infection
    SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-144771
    SARS-CoV-2-IN-14

    SARS-CoV Infection
    SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-146974
    PDE4-IN-9

    Phosphodiesterase (PDE) Inflammation/Immunology
    PDE4-IN-9 (Compound 5j) is a potent inhibitor of PDE4. PDE4-IN-9 exhibits lower IC50 value (1.4 μM) against PDE4 than parent rolipram (2.0 μM) in in vitro enzyme assay. PDE4-IN-9 also displays good in vivo activity in animal models of asthma/COPD and sepsis induced by LPS.
  • HY-144772
    SARS-CoV-2-IN-15

    SARS-CoV Infection
    SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally.
  • HY-150548
    COX-2/15-LOX-IN-1

    COX Lipoxygenase Inflammation/Immunology
    COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase enzyme (15-LOX) inhibitor with IC50 values of 10.65, 0.075 and 2.98 μM against COX-1, COX-2 and 15-LOX, respectively. COX-2/15-LOX-IN-1 shows anti-inflammatory activity.
  • 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-146410
    AT2R antagonist 1

    Angiotensin Receptor Others
    AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common drug-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.
  • HY-129039
    Butyrolactone 3

    MB-3

    Histone Acetyltransferase Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Butyrolactone 3 (MB-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). Butyrolactone 3 can be used in studies of cancer, metabolic, autoimmune and neurological diseases.
  • 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-N0492S
    α-Lipoic Acid-d5

    Thioctic acid-d5; (±)-α-Lipoic acid-d5; DL-α-Lipoic acid-d5

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid-d5 (Thioctic acid-d5) is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.
  • HY-108263A
    (S)-3-Hydroxy Midostaurin

    (S)-CGP52421

    FLT3 Drug Metabolite Cancer
    (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).
  • HY-N144101
    SARS-CoV MPro-IN-2

    SARS-CoV Infection
    SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 M pro with an IC50 value of 72.07 nM. The main protease (M pro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in drug discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19.
  • HY-146379
    SARS-CoV-2-IN-19

    SARS-CoV Infection
    SARS-CoV-2-IN-19 (Compound 6g) is a potent inhibitor of SARS-CoV-2 with an EC50 of 8.8 μM. SARS-CoV-2-IN-19 shows potent activity against SARS-CoV-2 helicase (nsp13), a highly conserved enzyme, highlighting a potentiality against emerging HCoVs outbreaks. SARS-CoV-2-IN-19 has the potential for the research of infection diseases.
  • HY-14393
    Emodin

    Frangula emodin

    SARS-CoV Casein Kinase Autophagy 11β-HSD Cancer
    Emodin (Frangula emodin), an anthraquinone derivative, 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-145384
    ROC-0929

    Phospholipase Inflammation/Immunology
    ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca 2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases.
  • 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-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-76779
    4-(Chloromethyl)-7-hydroxycoumarin

    Others Cancer
    4-(Chloromethyl)-7-hydroxycoumarin (compound 4) is a hydroxycoumarin derivative with potent antioxidant effect and high hydroxyl radical-scavenging property. 4-(Chloromethyl)-7-hydroxycoumarin contains a methyl group and a chlorine group in the heterocyclic ring. A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties has been investigated as potent inhibitors of the zinc enzyme carbonic anhydrase, expecially tumor-associated isoforms CA IX and XII.
  • HY-144381
    Glutamate-5-kinase-IN-1

    Others Infection
    Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents.
  • HY-125798
    2,3-Dehydro-2-deoxy-N-acetylneuraminic acid

    Neu5Ac2en; DANA

    Influenza Virus Infection
    N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid (Neu5Ac2en) is a potent neuraminidase (sialidase) inhibitor. N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid shows inhibitory activities against human neuraminidase enzymes with IC50s of 143, 43, 61, and 74 μM for NEU1, NEU2, NEU3, and NEU4, respectively. Anti-influenza virus activity.
  • HY-W011258
    H-Tyr-Phe-OH

    L-Tyrosyl-L-phenylalanine

    Xanthine Oxidase Angiotensin-converting Enzyme (ACE) Cancer Inflammation/Immunology
    H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells.
  • 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-145277
    SARS-CoV-2-IN-11

    SARS-CoV Infection
    SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals.
  • HY-101144
    RSM-932A

    TCD-717

    Others Cancer
    RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
  • 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-145276
    SARS-CoV-2-IN-10

    SARS-CoV Infection
    SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals.
  • HY-14280S2
    (E)-Entacapone-d10

    COMT Neurological Disease
    Entacapone-d10 is the deuterium labeled Entacapone. 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-14280S
    Entacapone-d10

    COMT Neurological Disease
    Entacapone-d10 is the deuterium labeled Entacapone. 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-142670
    Lp-PLA2-IN-5

    Phospholipase Metabolic Disease Neurological Disease
    Lp-PLA2-IN-5 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32).
  • HY-142669
    Lp-PLA2-IN-4

    Phospholipase Metabolic Disease Neurological Disease
    Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38).
  • HY-B0653
    Levobupivacaine

    (S)-(-)-Bupivacaine

    Sodium Channel Ferroptosis Cancer Neurological Disease
    Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-146755
    TIY-7

    Trk Receptor Cancer
    TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKA G595R, TRKA G667C, TRKA F589L, TRKC G623R, TRKC G696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model.
  • HY-B0653A
    Levobupivacaine hydrochloride

    (S)-(-)-Bupivacaine monohydrochloride

    Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-146000
    Influenza virus-IN-3

    Influenza Virus Inflammation/Immunology
    Influenza virus-IN-3 (compound 9) is a potent and selective influenza virus inhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM.
  • HY-144749
    AKR1C3-IN-5

    Others Cancer
    AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells.
  • 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-14393S
    Emodin-d4

    Frangula emodin-d4

    SARS-CoV Casein Kinase Autophagy 11β-HSD Cancer
    Emodin-d4 (Frangula emodin-d4) is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, 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-N0492
    α-Lipoic Acid

    Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
  • HY-142779
    Lp-PLA2-IN-11

    Phospholipase Metabolic Disease Neurological Disease
    Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).
  • HY-N0492A
    α-Lipoic Acid sodium

    Thioctic acid sodium; (±)-α-Lipoic acid sodium; DL-α-Lipoic acid sodium

    NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
  • 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-125961
    T3Inh-1

    Others Cancer
    T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).
  • 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-142778
    Lp-PLA2-IN-10

    Phospholipase Metabolic Disease Neurological Disease
    Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).
  • HY-146001
    Influenza virus-IN-4

    Influenza Virus Inflammation/Immunology
    Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice.
  • 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-122026
    PF-04802367

    PF-367

    GSK-3 Neurological Disease
    PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.