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Dehydrogenase Signaling Pathway Map

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Catalog No. Product Name Information Product Use Citations Product Validations
E0355New CVT-10216 CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM.
E1078New Emvododstat (PTC299) Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
S0209 BVT 2733 BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
S0522 CM10 CM10 is a potent and selective inhibitor of aldehyde dehydrogenase 1A family (ALDH1A) with IC50 of 1700 nM, 740 nM and 640 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively. CM10 exhibits anti-cancer activity.
S0718 AG-120 (racemic) AG-120 (racemic), the racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity.
Front Pharmacol, 2022, 13:871392
S0764 AKR1C1-IN-1 AKR1C1-IN-1 is a potent and selective inhibitor of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) with Ki of 4 nM, 87 nM, 4.2 μM and 18.2 μM for AKR1C1, AKR1C2, AKR1C3 and AKR1C4, respectively.
S1247 Leflunomide (HWA486) Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
Cell Death Dis, 2022, 13(2):154
Cell Death Dis, 2021, 12(9):821
Front Immunol, 2021, 12:685984
S1404 Trilostane Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
Invest New Drugs, 2021, 10.1007/s10637-021-01132-3
Oxid Med Cell Longev, 2019, 10.1155/2019/2985956
Proteomics, 2018, 18(23):e1800136
S1501 Mycophenolate mofetil (RS-61443) Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.
Clin Exp Rheumatol, 2021, N/A
Nat Commun, 2020, 11(1):3811
bioRxiv, 2020, 2020/9/20.4.7.30734
S1680 Disulfiram (NSC 190940) Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
Free Radic Biol Med, 2022, 181:14-28
mBio, 2022, 10.1128/mbio.02739-21
J Leukoc Biol, 2022, 10.1002/JLB.5MA1121-644R
S1717 Fomepizole Fomepizole (4-methylpyrazole, Antizol, Antizol-Vet) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
Oxid Med Cell Longev, 2019, 2019:3527809
Environ Mol Mutagen, 2019, 60(3):214-226
S2055 Gimeracil Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
Cancer Cell, 2021, S1535-6108(21)00659-0
S2289 Daidzin Daidzin (Daidzoside, Daidzein 7-O-glucoside, Daidzein 7-glucoside), a natural organic compound in the class of phytochemicals known as isoflavones, is a potent and selective inhibitor of human mitochondrial aldehyde dehydrogenase and inhibits ALDH-I selectively (Ki=20 nM); at least 500 times less effective against ALDH-Ⅱ, the cytosolic isozyme (Ki=10 μM).
S2295 Emodin Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Molecules, 2021, 26(5)1210
J Nutr Biochem, 2020, 79:108339
S2296 Enoxolone Enoxolone (Glycyrrhetin) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice.
J Med Virol, 2019, 91(8):1440-1447
S2302 Glycyrrhizin (NSC 167409) Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is a direct HMGB1(high mobility group box 1) inhibitor that inhibits HMGB1-dependent inflammatory molecule expression and oxidative stress; modulates P38 and P-JNK but not p-ERK signalling; Also inhibits 11 beta-hydroxysteroid dehydrogenase and monoamine oxidase (MAO).
Oxid Med Cell Longev, 2022, 2022:8438528
J Agric Food Chem, 2022, 70(9):2968-2983
Int Immunopharmacol, 2022, 108:108730
S2303 Gossypol Acetate Gossypol Acetate (Gossypol Acetic acid, Pogosin, AT101) is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.
J Agric Food Chem, 2022, 70(8):2589-2599
Cancers (Basel), 2021, 13(21)5579
Molecules, 2021, 26(5)1210
S2376 Ammonium Glycyrrhizinate Ammonium Glycyrrhizinate (AMGZ, Glycyram, Glycyrrhizin ammonium salt, Glycyrrhizic acid ammonium salt) is a unique product from Licorice root with a very high sweetness. Ammonium glycyrrhizinate is a direct inhibitor of HMGB1 with anti-inflammatory, anti-tumor, anti-diabetic activities. Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses. Ammonium Glycyrrhizinate also inhibits both hepatic delta 4-5-reductase and 11 beta-hydroxysteroid dehydrogenase.
S2487 Mycophenolic acid Mycophenolic acid (Mycophenolate, RS-61443) is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation.
Nat Commun, 2021, 12(1):1618
J Immunotoxicol, 2021, 18(1):154-162
ACS Infect Dis, 2020, acsinfecdis.0c00486
S2776 Devimistat (CPI-613) Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2.
Cell Mol Immunol, 2022, 10.1038/s41423-022-00842-9
J Exp Clin Cancer Res, 2021, 40(1):393
Front Immunol, 2021, 12:696101
S2987 4-Methyl-2-oxovaleric acid 4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity.
S3565 Brequinar Sodium Brequinar Sodium (Bipenquinate, BRQ, DUP-785, NSC 368390) is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of ~20 nM and triggers differentiation in the ER-HoxA9, U937, and THP1 cells with ED50 of ~1 μM.
S3574 IDH-305 IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively.
S3652 3-Nitropropionic acid 3-Nitropropionic acid (β-Nitropropionic Acid, 3-NP) is an irreversible inhibitor of mitochondrial respiratory Complex II succinate dehydrogenase, resulting in energy depletion through disruption of the electron transport chain.
Front Immunol, 2021, 12:618501
S3804 Alpha-Mangostin Alpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING.
Front Pharmacol, 2021, 12:692806
S3993 Ethyl Vanillate Ethyl vanillin (Bourbonal, Ethylprotal), a vanillin analog, is a flavouring agent and a fungicidal agent that exhibits strong antioxidant activity. Ethyl Vanillate inhibits 17β-HSD2 with an IC50 1.3 µM.
S4116 Isovaleramide Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
S4169 Teriflunomide Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
iScience, 2022, 25(5):104293
Molecules, 2021, 26(18)5653
J Gen Virol, 2021, 102(3)
S4805 Carboxine Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant. Carboxin inhibits succinate dehydrogenaseactivity .
S4900 Tenovin-6 Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2.
Front Immunol, 2021, 12:685523
Biomed Pharmacother, 2020, 125:109948
J Cell Sci, 2019, 132(6)
S4929 Enasidenib Mesylate Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).
Mol Cell, 2021, 81(18):3833-3847.e11
Cancer Res, 2021, 81(19):5033-5046
Yonsei Med J, 2020, 61(9):762-773
S5097 Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
Bioact Mater, 2022, 18:459-470
PLoS Comput Biol, 2022, 18(3):e1009395
Analyst, 2022, 10.1039/d2an00031h
S5146 3-Methylpyrazole 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
S5425 Phenylglyoxal hydrate Phenylglyoxal (1-Phenylethanedione) is a potent inhibitor of mitochondrial aldehyde dehydrogenase. It reacts with arginine residues in purified Hageman factor (HF, Factor XII) and causes inhibition of its coagulant properties.
S6626 Brequinar (DUP785) Brequinar (DUP785, NSC 368390) is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.
Adv Sci (Weinh), 2022, e2105451
iScience, 2022, 25(5):104293
bioRxiv, 2021, 10.1101/2021.06.28.450163
S6675 (R)-GNE-140 (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.
J Virol, 2022, jvi0197421
S6689 Merimepodib Merimepodib (Merimempodib, MMPD, VI-21,497, VX-497) is a potent, specific, and reversible inosine monophosphate dehydrogenase(IMPDH) inhibitor with antiviral activity against hepatitis C virus (HCV) and a variety of DNA and RNA viruses in vitro.Merimepodib is an immunosuppressive agent.
S6749 ASP-9521 ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5).
S6852 Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.
Mol Med Rep, 2021, 23(1)40
J Biol Chem, 2015, 290(34):20841-55
S7185 AGI-5198 AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
Cancer Res, 2022, 82(3):497-509
Proc Natl Acad Sci U S A, 2020, 5;117(18):9964-9972
Cancer Discov, 2020, CD-20-0226
S7241 AGI-6780 AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
J Hematol Oncol, 2022, 15(1):30
Stem Cells Int, 2022, 2022:1172795
Oncogene, 2021, 10.1038/s41388-021-01968-2
S7262 Vidofludimus Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
J Med Virol, 2022, 10.1002/jmv.27891
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S7900 SW033291 SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and Kiapp of 1.5 nM and 0.1 nM, respectively.
Nat Commun, 2022, 13(1):535
Elife, 2021, 10e70324
Pharmaceutics, 2021, 13(11)1934
S7941 NCT-501 NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
S8000 Tenovin-1 Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
J Pharm Biomed Anal, 2021, 201:114121
J Transl Med, 2019, 17(1):76
Sci Rep, 2019, 9(1):1897
S8205 Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
Mol Cell, 2021, S1097-2765(21)00507-4
Cancer Res, 2021, canres.1027.2021
iScience, 2021, 24(11):103350
S8206 Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
Nat Commun, 2022, 13(1):2614
Front Pharmacol, 2022, 13:871392
J Cancer, 2021, 12(16):4862-4872
S8382 ML390 ML390 is a human DHODH inhibitor with an IC50 of 0.56 μM and induces differentiation in acute myeloid leukemia.
J Med Virol, 2022, 10.1002/jmv.27891
S8405 RRx-001 RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.
Cell Mol Immunol, 2021, 18(6):1425-1436
Cancer Lett, 2021, 521:29-38
Cancer Lett, 2021, 521:29-38
S8530 BAY 1436032 BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants.
Haematologica, 2020, 2 pii: haematol
S8590 GSK 2837808A GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.
S8611 Vorasidenib (AG-881) Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).
Cell, 2019, 36(2):179-193
Cancer Cell, 2019, 36(2):179-193
S8615 Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.
Nat Commun, 2022, 13(1):1417
Mol Oncol, 2022, 16(1):219-249
J Exp Clin Cancer Res, 2021, 40(1):87
S8619 NCT-503 NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs.
Nat Immunol, 2022, 23(3):431-445
Nat Commun, 2022, 13(1):2698
Oxid Med Cell Longev, 2021, 2021:4232704
S8847 Orludodstat (BAY 2402234) Orludodstat (BAY 2402234) is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM.
iScience, 2022, 25(5):104293
bioRxiv, 2021, 10.1101/2021.06.28.450163
bioRxiv, 2021, 10.1101/2021.06.28.450163
S8881 DS-1001b (DS 1001) DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier.
S8949 Olutasidenib (FT-2102) Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.
S9617 G6PDi-1 G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.
S9645 CBR-5884 CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity.
S9721 ASLAN003

ASLAN003 (LAS 186323) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors.

iScience, 2022, 25(5):104293
bioRxiv, 2021, 10.1101/2021.06.28.450163
bioRxiv, 2021, 10.1101/2021.06.28.450163
S9776 AG-636 AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.
S9783 6-Aminonicotinamide 6-Aminonicotinamide (6AN) is an antimetabolite used to inhibit the NADPH-producing pentose phosphate pathway (PPP) in many cellular systems, making them more susceptible to oxidative stress. 6-Aminonicotinamide is a competitive inhibitor of NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) with Ki of 0.46 μM.
Cancer Metab, 2020, 8:19
S5800 Alda 1 Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2.
Front Med (Lausanne), 2022, 9:892472
E0355New CVT-10216 CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM.
E1078New Emvododstat (PTC299) Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
S0209 BVT 2733 BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
S0522 CM10 CM10 is a potent and selective inhibitor of aldehyde dehydrogenase 1A family (ALDH1A) with IC50 of 1700 nM, 740 nM and 640 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively. CM10 exhibits anti-cancer activity.
S0718 AG-120 (racemic) AG-120 (racemic), the racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity.
Front Pharmacol, 2022, 13:871392
S0764 AKR1C1-IN-1 AKR1C1-IN-1 is a potent and selective inhibitor of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) with Ki of 4 nM, 87 nM, 4.2 μM and 18.2 μM for AKR1C1, AKR1C2, AKR1C3 and AKR1C4, respectively.
S1247 Leflunomide (HWA486) Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
Cell Death Dis, 2022, 13(2):154
Cell Death Dis, 2021, 12(9):821
Front Immunol, 2021, 12:685984
S1404 Trilostane Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
Invest New Drugs, 2021, 10.1007/s10637-021-01132-3
Oxid Med Cell Longev, 2019, 10.1155/2019/2985956
Proteomics, 2018, 18(23):e1800136
S1501 Mycophenolate mofetil (RS-61443) Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.
Clin Exp Rheumatol, 2021, N/A
Nat Commun, 2020, 11(1):3811
bioRxiv, 2020, 2020/9/20.4.7.30734
S1680 Disulfiram (NSC 190940) Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
Free Radic Biol Med, 2022, 181:14-28
mBio, 2022, 10.1128/mbio.02739-21
J Leukoc Biol, 2022, 10.1002/JLB.5MA1121-644R
S1717 Fomepizole Fomepizole (4-methylpyrazole, Antizol, Antizol-Vet) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
Oxid Med Cell Longev, 2019, 2019:3527809
Environ Mol Mutagen, 2019, 60(3):214-226
S2055 Gimeracil Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
Cancer Cell, 2021, S1535-6108(21)00659-0
S2289 Daidzin Daidzin (Daidzoside, Daidzein 7-O-glucoside, Daidzein 7-glucoside), a natural organic compound in the class of phytochemicals known as isoflavones, is a potent and selective inhibitor of human mitochondrial aldehyde dehydrogenase and inhibits ALDH-I selectively (Ki=20 nM); at least 500 times less effective against ALDH-Ⅱ, the cytosolic isozyme (Ki=10 μM).
S2295 Emodin Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Molecules, 2021, 26(5)1210
J Nutr Biochem, 2020, 79:108339
S2296 Enoxolone Enoxolone (Glycyrrhetin) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice.
J Med Virol, 2019, 91(8):1440-1447
S2302 Glycyrrhizin (NSC 167409) Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is a direct HMGB1(high mobility group box 1) inhibitor that inhibits HMGB1-dependent inflammatory molecule expression and oxidative stress; modulates P38 and P-JNK but not p-ERK signalling; Also inhibits 11 beta-hydroxysteroid dehydrogenase and monoamine oxidase (MAO).
Oxid Med Cell Longev, 2022, 2022:8438528
J Agric Food Chem, 2022, 70(9):2968-2983
Int Immunopharmacol, 2022, 108:108730
S2303 Gossypol Acetate Gossypol Acetate (Gossypol Acetic acid, Pogosin, AT101) is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.
J Agric Food Chem, 2022, 70(8):2589-2599
Cancers (Basel), 2021, 13(21)5579
Molecules, 2021, 26(5)1210
S2376 Ammonium Glycyrrhizinate Ammonium Glycyrrhizinate (AMGZ, Glycyram, Glycyrrhizin ammonium salt, Glycyrrhizic acid ammonium salt) is a unique product from Licorice root with a very high sweetness. Ammonium glycyrrhizinate is a direct inhibitor of HMGB1 with anti-inflammatory, anti-tumor, anti-diabetic activities. Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses. Ammonium Glycyrrhizinate also inhibits both hepatic delta 4-5-reductase and 11 beta-hydroxysteroid dehydrogenase.
S2487 Mycophenolic acid Mycophenolic acid (Mycophenolate, RS-61443) is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation.
Nat Commun, 2021, 12(1):1618
J Immunotoxicol, 2021, 18(1):154-162
ACS Infect Dis, 2020, acsinfecdis.0c00486
S2776 Devimistat (CPI-613) Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2.
Cell Mol Immunol, 2022, 10.1038/s41423-022-00842-9
J Exp Clin Cancer Res, 2021, 40(1):393
Front Immunol, 2021, 12:696101
S2987 4-Methyl-2-oxovaleric acid 4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity.
S3565 Brequinar Sodium Brequinar Sodium (Bipenquinate, BRQ, DUP-785, NSC 368390) is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of ~20 nM and triggers differentiation in the ER-HoxA9, U937, and THP1 cells with ED50 of ~1 μM.
S3574 IDH-305 IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively.
S3652 3-Nitropropionic acid 3-Nitropropionic acid (β-Nitropropionic Acid, 3-NP) is an irreversible inhibitor of mitochondrial respiratory Complex II succinate dehydrogenase, resulting in energy depletion through disruption of the electron transport chain.
Front Immunol, 2021, 12:618501
S3804 Alpha-Mangostin Alpha-mangostin is the main xanthone purified from mangosteen and has health promoting benefits including anti-bacterial, anti-inflammatory, anti-oxidant, anti-cancer and cardioprotective activities. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM. Alpha-mangostin is also an agonist of human STING.
Front Pharmacol, 2021, 12:692806
S3993 Ethyl Vanillate Ethyl vanillin (Bourbonal, Ethylprotal), a vanillin analog, is a flavouring agent and a fungicidal agent that exhibits strong antioxidant activity. Ethyl Vanillate inhibits 17β-HSD2 with an IC50 1.3 µM.
S4116 Isovaleramide Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
S4169 Teriflunomide Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
iScience, 2022, 25(5):104293
Molecules, 2021, 26(18)5653
J Gen Virol, 2021, 102(3)
S4805 Carboxine Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant. Carboxin inhibits succinate dehydrogenaseactivity .
S4900 Tenovin-6 Tenovin-6 is a small molecule activator of p53 transcriptional activity and inhibits dihydroorotate dehydrogenase (DHODH). Tenovin-6 is also an inhibitor of SirT1 and SirT2.
Front Immunol, 2021, 12:685523
Biomed Pharmacother, 2020, 125:109948
J Cell Sci, 2019, 132(6)
S4929 Enasidenib Mesylate Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).
Mol Cell, 2021, 81(18):3833-3847.e11
Cancer Res, 2021, 81(19):5033-5046
Yonsei Med J, 2020, 61(9):762-773
S5097 Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.
Bioact Mater, 2022, 18:459-470
PLoS Comput Biol, 2022, 18(3):e1009395
Analyst, 2022, 10.1039/d2an00031h
S5146 3-Methylpyrazole 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
S5425 Phenylglyoxal hydrate Phenylglyoxal (1-Phenylethanedione) is a potent inhibitor of mitochondrial aldehyde dehydrogenase. It reacts with arginine residues in purified Hageman factor (HF, Factor XII) and causes inhibition of its coagulant properties.
S6626 Brequinar (DUP785) Brequinar (DUP785, NSC 368390) is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.
Adv Sci (Weinh), 2022, e2105451
iScience, 2022, 25(5):104293
bioRxiv, 2021, 10.1101/2021.06.28.450163
S6675 (R)-GNE-140 (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.
J Virol, 2022, jvi0197421
S6689 Merimepodib Merimepodib (Merimempodib, MMPD, VI-21,497, VX-497) is a potent, specific, and reversible inosine monophosphate dehydrogenase(IMPDH) inhibitor with antiviral activity against hepatitis C virus (HCV) and a variety of DNA and RNA viruses in vitro.Merimepodib is an immunosuppressive agent.
S6749 ASP-9521 ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5).
S6852 Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.
Mol Med Rep, 2021, 23(1)40
J Biol Chem, 2015, 290(34):20841-55
S7185 AGI-5198 AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
Cancer Res, 2022, 82(3):497-509
Proc Natl Acad Sci U S A, 2020, 5;117(18):9964-9972
Cancer Discov, 2020, CD-20-0226
S7241 AGI-6780 AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
J Hematol Oncol, 2022, 15(1):30
Stem Cells Int, 2022, 2022:1172795
Oncogene, 2021, 10.1038/s41388-021-01968-2
S7262 Vidofludimus Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
J Med Virol, 2022, 10.1002/jmv.27891
Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S7900 SW033291 SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and Kiapp of 1.5 nM and 0.1 nM, respectively.
Nat Commun, 2022, 13(1):535
Elife, 2021, 10e70324
Pharmaceutics, 2021, 13(11)1934
S7941 NCT-501 NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
S8000 Tenovin-1 Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
J Pharm Biomed Anal, 2021, 201:114121
J Transl Med, 2019, 17(1):76
Sci Rep, 2019, 9(1):1897
S8205 Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
Mol Cell, 2021, S1097-2765(21)00507-4
Cancer Res, 2021, canres.1027.2021
iScience, 2021, 24(11):103350
S8206 Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
Nat Commun, 2022, 13(1):2614
Front Pharmacol, 2022, 13:871392
J Cancer, 2021, 12(16):4862-4872
S8382 ML390 ML390 is a human DHODH inhibitor with an IC50 of 0.56 μM and induces differentiation in acute myeloid leukemia.
J Med Virol, 2022, 10.1002/jmv.27891
S8405 RRx-001 RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.
Cell Mol Immunol, 2021, 18(6):1425-1436
Cancer Lett, 2021, 521:29-38
Cancer Lett, 2021, 521:29-38
S8530 BAY 1436032 BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants.
Haematologica, 2020, 2 pii: haematol
S8590 GSK 2837808A GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.
S8611 Vorasidenib (AG-881) Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).
Cell, 2019, 36(2):179-193
Cancer Cell, 2019, 36(2):179-193
S8615 Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.
Nat Commun, 2022, 13(1):1417
Mol Oncol, 2022, 16(1):219-249
J Exp Clin Cancer Res, 2021, 40(1):87
S8619 NCT-503 NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs.
Nat Immunol, 2022, 23(3):431-445
Nat Commun, 2022, 13(1):2698
Oxid Med Cell Longev, 2021, 2021:4232704
S8847 Orludodstat (BAY 2402234) Orludodstat (BAY 2402234) is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM.
iScience, 2022, 25(5):104293
bioRxiv, 2021, 10.1101/2021.06.28.450163
bioRxiv, 2021, 10.1101/2021.06.28.450163
S8881 DS-1001b (DS 1001) DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier.
S8949 Olutasidenib (FT-2102) Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.
S9617 G6PDi-1 G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.
S9645 CBR-5884 CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity.
S9721 ASLAN003

ASLAN003 (LAS 186323) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors.

iScience, 2022, 25(5):104293
bioRxiv, 2021, 10.1101/2021.06.28.450163
bioRxiv, 2021, 10.1101/2021.06.28.450163
S9776 AG-636 AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.
S9783 6-Aminonicotinamide 6-Aminonicotinamide (6AN) is an antimetabolite used to inhibit the NADPH-producing pentose phosphate pathway (PPP) in many cellular systems, making them more susceptible to oxidative stress. 6-Aminonicotinamide is a competitive inhibitor of NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) with Ki of 0.46 μM.
Cancer Metab, 2020, 8:19
S5800 Alda 1 Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2.
Front Med (Lausanne), 2022, 9:892472
E0355New CVT-10216 CVT-10216 is a highly selective, reversible inhibitor of ALDH-2 with an IC50 of 29 nM.
E1078New Emvododstat (PTC299) Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM.
Tags: Dehydrogenase inhibition | Dehydrogenase activity | Dehydrogenase assay | Dehydrogenase reaction | Dehydrogenase enzyme activity | pyruvate dehydrogenase inhibition | pyruvate dehydrogenase activity | pyruvate dehydrogenase assay | pyruvate dehydrogenase phosphorylation | pyruvate dehydrogenase cancer | pyruvate dehydrogenase pathway | pyruvate dehydrogenase activation | dihydropyrimidine dehydrogenase activity | stearoyl-CoA desaturase pathway | Dehydrogenase inhibitor review