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Results for "11β-Hydroxysteroid Dehydrogenase Inhibitors" in MCE Product Catalog:

134

Inhibitors & Agonists

1

Screening Libraries

1

Dye Reagents

2

Biochemical Assay Reagents

33

Natural
Products

6

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-18055
    BVT-14225

    Others Metabolic Disease
    BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
  • HY-N2337
    11beta-Hydroxyprogesterone

    11β-Hydroxyprogesterone

    Endogenous Metabolite Cardiovascular Disease
    11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
  • HY-129630
    Tetrahydrocortisol

    Endogenous Metabolite Metabolic Disease
    Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity.
  • HY-101930
    BMS-816336

    Others Metabolic Disease
    BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
  • HY-101930B
    (R)-BMS-816336

    Others Metabolic Disease
    (R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
  • HY-18173
    AZD8329

    Others Metabolic Disease
    AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
  • HY-18056
    PF-915275

    Others Metabolic Disease
    PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.
  • HY-114464
    11-Beta-hydroxyandrostenedione

    4-Androsten-11β-ol-3,17-dione

    Endogenous Metabolite Endocrinology
    11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
  • HY-113165A
    Isobutyryl-L-carnitine chloride

    Endogenous Metabolite Others
    Isobutyryl-L-carnitine chloride is a product of the acyl-CoA dehydrogenases.
  • 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-B1877
    Nitrofen

    Others Cancer
    Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-135658
    hDHODH-IN-1

    Lactate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect.
  • HY-114702
    M77976

    PDHK Metabolic Disease
    M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes.
  • HY-76006
    3-Hydroxybenzaldehyde

    Aldehyde Dehydrogenase (ALDH) Cardiovascular Disease
    3-Hydroxybenzaldehyde is a precursor compound for phenolic compounds, such as Protocatechualdehyde (HY-N0295). 3-Hydroxybenzaldehyde is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans (ALDH2). 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo.
  • HY-113013
    Hydroxypyruvic acid

    β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid

    Endogenous Metabolite Metabolic Disease
    Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
  • HY-135841
    CM10

    Aldehyde Dehydrogenase (ALDH) Cancer Metabolic Disease
    CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity.
  • HY-113013A
    Hydroxypyruvic acid lithium hydrate

    β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate

    Endogenous Metabolite Metabolic Disease
    Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
  • HY-113165
    Isobutyryl-L-carnitine

    Endogenous Metabolite Metabolic Disease
    Isobutyryl-L-carnitine is a product of the acyl-CoA dehydrogenases.
  • HY-W007330
    2-Bromoacetamide

    Others Metabolic Disease
    2-Bromoacetamide can inactivate alcohol dehydrogenase.
  • HY-113076
    Thiamine pyrophosphate

    Endogenous Metabolite Metabolic Disease
    Thiamine pyrophosphate is the coenzyme form of Vitamin B1 and is a required intermediate in the pyruvate dehydrogenase complex and the ketoglutarate dehydrogenase complex.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-15453
    Devimistat

    CPI-613

    Apoptosis Cancer
    Devimistat (CPI-613) is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.
  • HY-12688
    Succinyl phosphonate

    Others Others
    Succinyl phosphonate is an inhibitor of the α-ketoglutarate dehydrogenase.
  • HY-101603
    Manitimus

    FK778

    Others Inflammation/Immunology
    Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive drug.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-115292
    Simvastatin hydroxy acid sodium

    Tenivastatin sodium; Simvastatin Impurity A sodium

    HMG-CoA Reductase (HMGCR) Cancer
    Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
  • HY-N1177
    Taraxerone

    Aldehyde Dehydrogenase (ALDH) Inflammation/Immunology
    Taraxerone is isolated from Sedum sarmentosum. Taraxerone enhances effects on alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) activities with EC50 values of 512.42 and 500.16 μM, respectively.
  • HY-129545
    DS-1001b

    Isocitrate Dehydrogenase (IDH) Cancer
    DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.
  • HY-N2498
    Glomeratose A

    Lactate Dehydrogenase Others
    Glomeratose A is a lactate dehydrogenase inhibitor, isolated from Polygala tenuifolia.
  • HY-B0083
    Leflunomide

    HWA486; RS-34821; SU101

    Others Cancer
    Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
  • HY-101966
    NCT-503

    Others Cancer
    NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
  • HY-112645
    BAY-2402234

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
  • HY-100020
    BAY-1436032

    Isocitrate Dehydrogenase (IDH) Cancer
    BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-B0876
    Fomepizole

    4-Methylpyrazole

    Others Others
    Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase which plays a key role in the metabolism of ethylene glycol and methanol.
  • HY-14281
    Trilostane

    Win 24540

    Others Endocrinology Cancer
    Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
  • HY-77521
    Dabigatran ethyl ester hydrochloride

    Thrombin Cardiovascular Disease
    Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor.
  • HY-100742B
    (S)-GNE-140

    Lactate Dehydrogenase Cancer
    (S)-GNE-140 is the less active enantiomer of GNE-140 which can inhibit Lactate dehydrogenase A (LDHA).
  • HY-13986
    Merimepodib

    VX-497; MMPD

    HBV HCV Infection
    Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
  • HY-W051723
    (R)-3-Hydroxybutanoic acid

    Endogenous Metabolite Others
    (R)-3-Hydroxybutanoic acid is a metabolite, and converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-18768
    NCT-501

    Aldehyde Dehydrogenase (ALDH) Cancer
    NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
  • HY-124062
    TAS-114

    Others Cancer
    TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.
  • HY-119459
    Fluopyram

    Fungal Infection
    Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
  • HY-17469
    Gimeracil

    Gimestat

    Others Cancer
    Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.
  • HY-W014787
    Decanedioic acid

    Endogenous Metabolite Metabolic Disease
    Decanedioic acid, a normal urinary acid, is found to be associated with carnitine-acylcarnitine translocase deficiency and medium chain acyl-CoA dehydrogenase deficiency.
  • HY-W012530
    2-Oxo-3-phenylpropanoic acid

    Endogenous Metabolite Others
    2-Oxo-3-phenylpropanoic acid is used in the synthesis of 3-phenyllactic acid (PLA) by lactate dehydrogenase.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-100681
    GSK2837808A

    Lactate Dehydrogenase Cancer
    GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 1.9 and 14 nM for LDHA and LDHB, respectively.
  • HY-103096
    R162

    Others Cancer
    R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
  • HY-111095
    D-(-)-Lactic acid

    (R)-2-Hydroxypropionic acid

    Endogenous Metabolite Metabolic Disease
    D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants.
  • HY-N2597
    Prunetin

    Aldehyde Dehydrogenase (ALDH) Inflammation/Immunology
    Prunetin, an O-methylated isoflavone, possesses anti-inflammatory activity. Prunetin is a potent human aldehyde dehydrogenases inhibitor.
  • HY-19801
    CVT-10216

    Aldehyde Dehydrogenase (ALDH) Neurological Disease
    CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.
  • HY-N6736
    K-252c

    PKC Bacterial Apoptosis Cancer Infection
    K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.
  • HY-18768A
    NCT-501 hydrochloride

    Aldehyde Dehydrogenase (ALDH) Cancer
    NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
  • HY-B0199
    Mycophenolate Mofetil

    RS 61443; TM-MMF

    Apoptosis Cancer
    Mycophenolate Mofetil is an immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) with IC50s of 39 nM and 27 nM, respectively.
  • HY-111108
    LDH-IN-1

    Lactate Dehydrogenase Cancer
    LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively.
  • HY-135570
    DHODH-IN-2

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus Infection
    DHODH-IN-2 (compound 21d) is a human dihydroorotate dehydrogenase (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC50 value of 8.6.
  • HY-113304
    (S)-3,4-Dihydroxybutyric acid

    Endogenous Metabolite Metabolic Disease
    (S)-3,4-Dihydroxybutyric acid is a normal human urinary metabolite that is excreted in increased concentration in patients with succinic semialdehyde dehydrogenase (SSADH) deficiency.
  • HY-16214
    FX-11

    LDHA Inhibitor FX11

    Lactate Dehydrogenase Cancer
    FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell,a Ki value of 8 μM.
  • HY-108325
    Brequinar

    DUP785; NSC 368390

    Dihydroorotate Dehydrogenase Virus Protease DNA/RNA Synthesis Cancer Infection Inflammation/Immunology
    Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses.
  • HY-113128
    sn-Glycerol 3-phosphate

    Endogenous Metabolite Others
    sn-Glycerol 3-phosphate is produced by cytosolic glycerol 3-phosphate dehydrogenase pathway through the reduction of dihydroxyacetone phosphate using NADH formed during glycolysis.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-12688A
    Succinyl phosphonate trisodium salt

    Endogenous Metabolite Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-113166
    Dodecanoylcarnitine

    Endogenous Metabolite Metabolic Disease
    Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease.
  • HY-122577
    EN40

    Aldehyde Dehydrogenase (ALDH) Cancer
    EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM
  • HY-N7114A
    Chloramphenicol succinate sodium

    Bacterial Antibiotic Metabolic Disease Infection
    Chloramphenicol succinate sodium is a prodrug of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity.
  • HY-113128B
    sn-Glycerol 3-phosphate biscyclohexylammonium salt

    Endogenous Metabolite Metabolic Disease
    sn-Glycerol 3-phosphate biscyclohexylammonium salt is produced by cytosolic glycerol 3-phosphate dehydrogenase pathway through the reduction of dihydroxyacetone phosphate using NADH formed during glycolysis.
  • HY-18717
    Mutant IDH1-IN-2

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
  • HY-W040073
    Nifurtimox

    Parasite Lactate Dehydrogenase Cancer Infection
    Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
  • HY-113212
    Ursocholic acid

    Endogenous Metabolite Metabolic Disease
    Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
  • HY-N0018
    Daidzin

    Daidzoside; NPI-031D; Daidzein 7-O-glucoside

    Mitochondrial Metabolism Reverse Transcriptase Others
    Daidzin is an isoflavone that has anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC50 = 80 nM) and is an effective anti-dipsotropic isoflavone.
  • HY-128578
    KPLH1130

    PDHK Metabolic Disease Inflammation/Immunology
    KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.
  • HY-100742
    GNE-140 racemate

    Lactate Dehydrogenase Cancer
    GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor.
  • HY-135654
    hDHODH-IN-2

    Lactate Dehydrogenase DNA/RNA Synthesis Inflammation/Immunology
    hDHODH-IN-2 is an analogue of the active metabolite of Leflunomide. hDHODH-IN-2 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory activity.
  • HY-128787
    DHODH-IN-5

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus Infection
    DHODH-IN-5 is a potent human dihydroorotate dehydrogenase (DHODH) inhibitor, with a pIC50 of 7.8 for human recombinant DHODH. DHODH-IN-5 inhibits measles virus replication, with a pMIC50 of 8.8.
  • HY-N3115
    Palbinone

    Others Inflammation/Immunology
    Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity.
  • HY-W012875
    3-Nitropropanoic acid

    β-Nitropropionic acid; Bovinocidin

    Bacterial Apoptosis Infection Metabolic Disease
    3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-135648
    PfDHODH-IN-1

    Parasite Lactate Dehydrogenase DNA/RNA Synthesis Infection
    PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity.
  • HY-117240
    NCT-502

    Others Cancer
    NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH.
  • HY-16082
    AZD7545

    PDHK Metabolic Disease
    AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
  • HY-136594
    BODIPY aminoacetaldehyde

    BAAA

    Aldehyde Dehydrogenase (ALDH) Cancer
    BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
  • HY-W017522
    Adipic acid

    Endogenous Metabolite Metabolic Disease
    Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.
  • HY-W016645
    4-Diethylaminobenzaldehyde

    Aldehyde Dehydrogenase (ALDH) Cancer
    4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM).
  • HY-136498
    T-705RMP

    Drug Metabolite Infection
    T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM.
  • HY-101943
    LY 345899

    Others Cancer
    LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC50 values of 96 nM and 663 nM, respectively and a Ki of 18 nM for MTHFD1.
  • HY-100742A
    (R)-GNE-140

    Lactate Dehydrogenase Cancer
    (R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
  • HY-113108
    (R)-3-Hydroxyisobutyric acid

    Endogenous Metabolite Metabolic Disease
    (R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-123962
    G6PD activator AG1

    Others Metabolic Disease
    G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ, extracted from patent WO2019023264A1, compound AG1.
  • HY-19540
    GSK864

    Isocitrate Dehydrogenase (IDH) Cancer
    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  • HY-114009
    AKR1C1-IN-1

    Others Neurological Disease
    AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1.
  • HY-12492
    VER-246608

    PDHK Cancer
    VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
  • HY-100184
    DSM265

    Parasite Infection
    DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC50 of 4.3 nM.
  • HY-10533
    Eniluracil

    5-Ethynyluracil; GW776C85

    Others Cancer
    Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
  • HY-Y0445A
    Sodium dichloroacetate

    PDHK Reactive Oxygen Species NKCC Apoptosis Cancer
    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-109619
    D4-abiraterone

    Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite

    Androgen Receptor Cytochrome P450 Cancer
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
  • HY-103394
    TC HSD 21

    Others Cancer
    TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
  • HY-B1729
    Phenoxyethanol

    Bacterial Infection
    Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.
  • HY-126241
    RV01

    Aldehyde Dehydrogenase (ALDH) Inflammation/Immunology
    RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
  • HY-N2177
    3-Dehydrotrametenolic acid

    Lactate Dehydrogenase Apoptosis Cancer
    3-​Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-​Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-​Dehydrotrametenolic acid induces apoptosis and has anticancer activity.
  • HY-114459
    Mutant IDH1-IN-4

    Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
  • HY-126254
    BI-4924

    Others Cancer
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
  • HY-N7393
    Isomalt

    Palatinitol

    Lactate Dehydrogenase Metabolic Disease
    Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-129239
    ASLAN003

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Apoptosis Cancer
    ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
  • HY-B0240
    Disulfiram

    Tetraethylthiuram disulfide; TETD

    Aldehyde Dehydrogenase (ALDH) Interleukin Related Metabolic Disease Cancer
    Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
  • HY-113377
    L-Glyceric acid

    Endogenous Metabolite Metabolic Disease
    L-Glyceric acid is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid excretion to distinguish PH1 from PH2.
  • HY-113377A
    L-Glyceric acid sodium

    Endogenous Metabolite Metabolic Disease
    L-Glyceric acid sodium is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid sodium can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid sodium excretion to distinguish PH1 from PH2.
  • HY-130251
    DS18561882

    Others Cancer
    DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile.
  • HY-13423
    Tenovin-1

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.
  • 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-10545
    Taribavirin

    HBV HCV Infection
    Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
  • HY-10545A
    Taribavirin hydrochloride

    HBV HCV Infection
    Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
  • HY-100012
    CBR-5884

    Others Cancer
    CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.
  • HY-135954A
    PDK4-IN-1 hydrochloride

    PDHK Apoptosis Cancer Metabolic Disease Inflammation/Immunology
    PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
  • HY-N0108
    Physcion

    Parietin; Rheochrysidin

    Bacterial Cancer Infection Inflammation/Immunology
    Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.
  • HY-101813
    Laflunimus

    HR325

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Prostaglandin Receptor Inflammation/Immunology
    Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.
  • HY-114855
    BT2

    Bcl-2 Family Metabolic Disease
    BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.
  • HY-15510B
    Tenovin-6 Hydrochloride

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
  • HY-15510
    Tenovin-6

    MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy Cancer
    Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
  • HY-13653
    (-)-Epigallocatechin Gallate

    EGCG; Epigallocatechol Gallate

    Autophagy Reactive Oxygen Species HIV Ferroptosis Mitochondrial Metabolism Endogenous Metabolite Cancer
    (-)-Epigallocatechin Gallate is a tea flavonoid with potent antioxidant, antiinflammatory, and anticarcinogenic properties. (-)-Epigallocatechin Gallate is reported to inhibit EGFR signaling and thereby exert anticancer effects. (-)-Epigallocatechin Gallate (EGCG) is a glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) inhibitor. Epigallocatechin-3-gallate induces oxidative phosphorylation (OXPHOS) by activating cytochrome c oxidase.
  • HY-B0968A
    Trimetazidine

    Autophagy Cardiovascular Disease
    Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
  • HY-114226
    Olutasidenib

    FT-2102

    Isocitrate Dehydrogenase (IDH) Cancer Inflammation/Immunology
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
  • HY-B0968
    Trimetazidine dihydrochloride

    Autophagy Cardiovascular Disease
    Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
  • HY-113466
    4-Hydroxynonenal

    4-HNE

    Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite Cancer Neurological Disease Cardiovascular Disease
    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
  • HY-121744
    PS10

    PDHK Inflammation/Immunology
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
  • HY-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.