Dehydrogenase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

ALDH1A Selective

Dehydrogenase Products

All (61) Dehydrogenase Inhibitors (60) Dehydrogenase Agonists (1)

Catalog No.	Information	Product Use Citations	Product Validations
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	Natural killer cell activation is differentially modulated by treatment with CsA,Tac, Sir, or MMF. PBMC of three or four healthy donors were incubated for 4 days with or without 500 U/ml IL-2 in the presence CNI (CsA and Tac), mTORi (Sir), or mycophenolate (MMF) at a concentration of 10 µM, DMSO control solvent or medium.The percentage of CD25+ NK cells were determined by ﬂow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.
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.	Front Immunol, 2021, 12:696101 Elife, 2020, 9e56749 J Exp Clin Cancer Res, 2020, 28;39(1):73
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.	Gastroenterology, 2019, 10.1053/j Sci Rep, 2019, 9(1):3462 Toxicol Lett, 2018, 282:154-165	Peritoneal macrophages were pretreated for 1 h with the leﬂunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, ^#P < 0.05 versus rTsP53 group.
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 ACS Infect Dis, 2020, acsinfecdis.0c00486 Viruses, 2020, 12(10)E1067
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.	Proc Natl Acad Sci U S A, 2020, 5;117(18):9964-9972 Cancer Discov, 2020, CD-20-0226 Oncol Lett, 2020, 19(2):1322-1330	AGI-5198 restored p53 expression in HCT116 cells harboring IDH1 R132H mutant. HCT116 cells were infected with control lentivirus or lentivirus expressing Flag-WT IDH1 or IDH1-R132H. At 48 hr post-infection, cells were treated with or without 1.5 μM AGI-5198 for 2 days, followed by treating with 2.5 M DOX (or not) for another 9 hr in the presence of AGI-5198, as indicated.
S9776^New	AG-636 AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.
S4929^New	Enasidenib Mesylate Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).
S3565^New	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^New	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 IDH1^R132H, IDH1^R132C and IDH1^WT, respectively.
S9783^New	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.
S9721^New	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.
S2987^New	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.
S6852^New	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
S9645^New	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.
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).	Elife, 2021, 10e63810 mBio, 2021, 12(1)e02754-20 J Infect Chemother, 2021, 27(5):696-701	The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “” for p<0.05 or “*” for p<0.01.
S1404	Trilostane Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.	Oxid Med Cell Longev, 2019, 10.1155/2019/2985956 Proteomics, 2018, 18(23):e1800136 Biochim Biophys Acta Mol Cell Biol Lipids, 2018, 1863(6):625-638	Long-time incubations. Spine number in calbindin-labeled PC (red, 7 div) in controls (a), after MLTI (b), MLTI combined with AG205 (c), and MLTI plus trilostane (d); 4d 4 days. Analysis of PC spine number in cell cultures treated with mifepristone in combination with progesterone, AG205, and trilostane at different developmental ages.
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	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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.	J Gen Virol, 2021, 102(3) Mol Cell, 2020, 80(6):1104-1122.e9 Neuroscience, 2020, 428:228-241	Leflunomide or teriflunomide were incubated with H1299, H460, A549 cells at indicated concentrations for or 2, 4 or 6 days, followed by MTT assay.
S2055	Gimeracil Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
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.
S6749	ASP-9521 ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5).
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.
S8382	ML390 ML390 is a human DHODH inhibitor with an IC50 of 0.56 μM and induces differentiation in acute myeloid leukemia.
S5097	Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 J Clin Med, 2021, 10(7)1431 Int J Mol Sci, 2021, 22(3)1194
S5146	3-Methylpyrazole 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
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.
S8847	BAY 2402234 BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM.
S4116	Isovaleramide Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
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.
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.	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) Nat Biotechnol, 2015, 10.1038/nbt.3130
S7900	SW033291 SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and K_i^app of 1.5 nM and 0.1 nM, respectively.	J Clin Invest, 2020, 131554 Nat Commun, 2019, 10(1):181
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.
S7241	AGI-6780 AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.	Blood, 2018, 10.1182/blood-2018-05-850826 Theranostics, 2018, 8(15):4050-4061	Western blot of KMM-1 and NCI-H929 cells, UT, treated with DMSO, AGI-6780 (KMM-1: 5 μM; NCI-H929: 10 μM), CFZ (KMM-1: 5 nM; NCI-H929: 2.5 nM), or a combination of the 2 drugs. Cell lysates were immunoblotted using the indicated antibodies 24 hours posttreatment. Vinculin protein expression was included for protein loading normalization.
S7941	NCT-501 NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
S9617	G6PDi-1 G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.
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.
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
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).
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.	Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S2295	Emodin Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).	Molecules, 2021, 26(5)1210 J Nutr Biochem, 2020, 79:108339 Oncotarget, 2020, 11(46):4224-4242	Trypsin inhibition dose-response curves in the absence (black circles) and presence (red triangles) of detergent for (A) emodin.
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).	Cancer Sci, 2021, 112(4):1603-1613 Int Immunopharmacol, 2021, 98:107859 Biochem Biophys Res Commun, 2021, 536:100-106	Western blot analysis of TLR2 and CXCR4 after direct inhibition with glycyrrhizin.
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.	Molecules, 2021, 26(5)1210 Mol Med Rep, 2021, 23(1)40 Biomed Pharmacother, 2019, 115:108860	16h after seeding HMLE RAS cells were exposed to 5 uM or 10 uM Gossypol in the presence or absence of Cisplatin for 16h. Afterwards, cells were harvested and lysates were analyzed for apoptosis by western blotting. Actin staining was used as loading control, while LC3a/b staining was used as indicator for autophagy. Accumulation of LC3a/b II indicates autophagy. Non-treated and DMSO-treated cells were used as control. Arrows are indicating the intended staining. For Bcl-xL: * indicates deamidated protein, # indicates unmodified protein. n=1.
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.
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
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.	J Exp Clin Cancer Res, 2021, 40(1):87 Cancer Sci, 2021, 10.1111/cas.15055 Environ Toxicol, 2021, 10.1002/tox.23098
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
S8206	Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.	Journal of Cancer, 2021, 12(16): 4862-4872 Cancer Discov, 2019, 9(6):756-777 Drug Des Devel Ther, 2018, 12:1009-1017	(C) MGC-803 cells were treated with the control (DMEM culture), 1% alcohol (DMEM culture medium with 1% alcohol) and AG-120 (40, 60, 80 and 100 µM) for 24, 48 or 72 h.
S4805	Carboxine Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant. Carboxin inhibits succinate dehydrogenaseactivity .
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.	Elife, 2020, 9e56749
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.
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.
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.
S8205	Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.	Elife, 2020, 9e56749 Yonsei Med J, 2020, 61(9):762-773 Cancer Sci, 2019, 110(10):3306-3314
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.
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.
S0209	BVT 2733 BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
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.
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
S6626	Brequinar (DUP785) Brequinar (DUP785, NSC 368390) is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.
S5800	Alda 1 Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH21) and ALDH22.

Catalog No.	Information	Product Use Citations	Product Validations
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	Natural killer cell activation is differentially modulated by treatment with CsA,Tac, Sir, or MMF. PBMC of three or four healthy donors were incubated for 4 days with or without 500 U/ml IL-2 in the presence CNI (CsA and Tac), mTORi (Sir), or mycophenolate (MMF) at a concentration of 10 µM, DMSO control solvent or medium.The percentage of CD25+ NK cells were determined by ﬂow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.
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.	Front Immunol, 2021, 12:696101 Elife, 2020, 9e56749 J Exp Clin Cancer Res, 2020, 28;39(1):73
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.	Gastroenterology, 2019, 10.1053/j Sci Rep, 2019, 9(1):3462 Toxicol Lett, 2018, 282:154-165	Peritoneal macrophages were pretreated for 1 h with the leﬂunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, ^#P < 0.05 versus rTsP53 group.
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 ACS Infect Dis, 2020, acsinfecdis.0c00486 Viruses, 2020, 12(10)E1067
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.	Proc Natl Acad Sci U S A, 2020, 5;117(18):9964-9972 Cancer Discov, 2020, CD-20-0226 Oncol Lett, 2020, 19(2):1322-1330	AGI-5198 restored p53 expression in HCT116 cells harboring IDH1 R132H mutant. HCT116 cells were infected with control lentivirus or lentivirus expressing Flag-WT IDH1 or IDH1-R132H. At 48 hr post-infection, cells were treated with or without 1.5 μM AGI-5198 for 2 days, followed by treating with 2.5 M DOX (or not) for another 9 hr in the presence of AGI-5198, as indicated.
S9776^New	AG-636 AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.
S4929^New	Enasidenib Mesylate Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).
S3565^New	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^New	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 IDH1^R132H, IDH1^R132C and IDH1^WT, respectively.
S9783^New	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.
S9721^New	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.
S2987^New	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.
S6852^New	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
S9645^New	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.
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).	Elife, 2021, 10e63810 mBio, 2021, 12(1)e02754-20 J Infect Chemother, 2021, 27(5):696-701	The effect of drugs on sperm movement. Purified human sperm were incubated under capacitating conditions for 0, 15, 30, 60 or 120 min, and motility was measured in the presence of disulfirum. The standard deviation is shown as bars. Statistical differences by Student's t-test compared with control are annotated as “” for p<0.05 or “*” for p<0.01.
S1404	Trilostane Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.	Oxid Med Cell Longev, 2019, 10.1155/2019/2985956 Proteomics, 2018, 18(23):e1800136 Biochim Biophys Acta Mol Cell Biol Lipids, 2018, 1863(6):625-638	Long-time incubations. Spine number in calbindin-labeled PC (red, 7 div) in controls (a), after MLTI (b), MLTI combined with AG205 (c), and MLTI plus trilostane (d); 4d 4 days. Analysis of PC spine number in cell cultures treated with mifepristone in combination with progesterone, AG205, and trilostane at different developmental ages.
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	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
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.	J Gen Virol, 2021, 102(3) Mol Cell, 2020, 80(6):1104-1122.e9 Neuroscience, 2020, 428:228-241	Leflunomide or teriflunomide were incubated with H1299, H460, A549 cells at indicated concentrations for or 2, 4 or 6 days, followed by MTT assay.
S2055	Gimeracil Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
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.
S6749	ASP-9521 ASP-9521 is a selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17β-HSD5).
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.
S8382	ML390 ML390 is a human DHODH inhibitor with an IC50 of 0.56 μM and induces differentiation in acute myeloid leukemia.
S5097	Methotrexate disodium Methotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 J Clin Med, 2021, 10(7)1431 Int J Mol Sci, 2021, 22(3)1194
S5146	3-Methylpyrazole 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
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.
S8847	BAY 2402234 BAY 2402234 is a novel and selective dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 1.2 nM.
S4116	Isovaleramide Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
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.
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.	Biomed Pharmacother, 2020, 125:109948 J Cell Sci, 2019, 132(6) Nat Biotechnol, 2015, 10.1038/nbt.3130
S7900	SW033291 SW033291 is a selective inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) with IC50 and K_i^app of 1.5 nM and 0.1 nM, respectively.	J Clin Invest, 2020, 131554 Nat Commun, 2019, 10(1):181
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.
S7241	AGI-6780 AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.	Blood, 2018, 10.1182/blood-2018-05-850826 Theranostics, 2018, 8(15):4050-4061	Western blot of KMM-1 and NCI-H929 cells, UT, treated with DMSO, AGI-6780 (KMM-1: 5 μM; NCI-H929: 10 μM), CFZ (KMM-1: 5 nM; NCI-H929: 2.5 nM), or a combination of the 2 drugs. Cell lysates were immunoblotted using the indicated antibodies 24 hours posttreatment. Vinculin protein expression was included for protein loading normalization.
S7941	NCT-501 NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
S9617	G6PDi-1 G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.
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.
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
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).
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.	Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855
S2295	Emodin Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).	Molecules, 2021, 26(5)1210 J Nutr Biochem, 2020, 79:108339 Oncotarget, 2020, 11(46):4224-4242	Trypsin inhibition dose-response curves in the absence (black circles) and presence (red triangles) of detergent for (A) emodin.
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).	Cancer Sci, 2021, 112(4):1603-1613 Int Immunopharmacol, 2021, 98:107859 Biochem Biophys Res Commun, 2021, 536:100-106	Western blot analysis of TLR2 and CXCR4 after direct inhibition with glycyrrhizin.
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.	Molecules, 2021, 26(5)1210 Mol Med Rep, 2021, 23(1)40 Biomed Pharmacother, 2019, 115:108860	16h after seeding HMLE RAS cells were exposed to 5 uM or 10 uM Gossypol in the presence or absence of Cisplatin for 16h. Afterwards, cells were harvested and lysates were analyzed for apoptosis by western blotting. Actin staining was used as loading control, while LC3a/b staining was used as indicator for autophagy. Accumulation of LC3a/b II indicates autophagy. Non-treated and DMSO-treated cells were used as control. Arrows are indicating the intended staining. For Bcl-xL: * indicates deamidated protein, # indicates unmodified protein. n=1.
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.
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
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.	J Exp Clin Cancer Res, 2021, 40(1):87 Cancer Sci, 2021, 10.1111/cas.15055 Environ Toxicol, 2021, 10.1002/tox.23098
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
S8206	Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.	Journal of Cancer, 2021, 12(16): 4862-4872 Cancer Discov, 2019, 9(6):756-777 Drug Des Devel Ther, 2018, 12:1009-1017	(C) MGC-803 cells were treated with the control (DMEM culture), 1% alcohol (DMEM culture medium with 1% alcohol) and AG-120 (40, 60, 80 and 100 µM) for 24, 48 or 72 h.
S4805	Carboxine Carboxin (Carbathiin, Vitavax, Kisvax) is a systemic agricultural fungicide and seed protectant. Carboxin inhibits succinate dehydrogenaseactivity .
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.	Elife, 2020, 9e56749
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.
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.
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.
S8205	Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.	Elife, 2020, 9e56749 Yonsei Med J, 2020, 61(9):762-773 Cancer Sci, 2019, 110(10):3306-3314
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.
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.
S0209	BVT 2733 BVT 2733, a new small molecule, is a non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
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.
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
S6626	Brequinar (DUP785) Brequinar (DUP785, NSC 368390) is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.