Dehydrogenase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Dehydrogenase Products

All (36) Dehydrogenase Inhibitors (35) Dehydrogenase Agonists (1) New Dehydrogenase Products

Catalog No.	Information	Product Use Citations	Product Validations
S1501	Mycophenolate Mofetil Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.	Front Immunol, 2013, 4:46 Clin Immunol, 2016, 164:65-77	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 all NK cells (CD3− /CD56+ ) and of the major NK cell subsets deﬁned as CD16+ /CD16− CD56dim and CD56bright were determined by ﬂow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.
S2776	CPI-613 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. Phase 2.
S1247	Leflunomide Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.	J Proteomics, 2012, 79:114-22 Cell Immunol, 2014, 288(1-2):1-7 Toxicol Lett, 2018, 282:154-165	H1299, H460, A549 cells were treated with leflunomide or teriflunomide at indicated concentrations for 24 h.
S2487	Mycophenolic acid Mycophenolic acid is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation.	J Virol Methods, 2016, 238:13-20 Clin Immunol, 2016, 164:65-77
S7185	AGI-5198 AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.	J BIOL CHEM, 2018, 10.1074/jbc.RA117.001385	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.
S8530^New	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.
S1158	MK-8245 MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. Phase 2.
S1680	Disulfiram Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.	J Proteomics, 2012, 79:114-22 Biofabrication, 2018, 10(4):044102	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 is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.	Cell Mol Life Sci, 2014, 71(9):1723-40 J Mol Endocrinol, 2014, 53(2):175-90 Biol Reprod, 2012, 87(2):35	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.
S4169	Teriflunomide Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.	Toxicol Lett, 2018, 282:154-165	Leflunomide or teriflunomide were incubated with H1299, H460, A549 cells at indicated concentrations for or 2, 4 or 6 days, followed by MTT assay.
S8076	PluriSIn #1 (NSC 14613) PluriSIn #1 is an inhibitor of the stearoyl-coA desaturase 1 (SCD1), which is able to selectively eliminate hPSCs.
S2376	Ammonium Glycyrrhizinate Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses.
S2055	Gimeracil Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
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.
S5146	3-Methylpyrazole 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
S4116	Isovaleramide Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
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.
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.
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.
S2289	Daidzin Daidzin, 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 is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Phase 2.
S2295	Emodin Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).	Mol Nutr Food Res, 2017, 10.1002/mnfr.201600744 ACS Chem Biol, 2015, 10.1021/cb5009487 Food Chem Toxicol, 2013, 55:363-70	Trypsin inhibition dose-response curves in the absence (black circles) and presence (red triangles) of detergent for (A) emodin.
S2296	Enoxolone Enoxolone is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice.
S2302	Glycyrrhizin (Glycyrrhizic Acid) Glycyrrhizin (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).	DNA Cell Biol, 2017, 36(1):67-76	Western blot analysis of TLR2 and CXCR4 after direct inhibition with glycyrrhizin.
S2303	gossypol-Acetic acid Gossypol Acetate is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.	Pigment Cell Melanoma Res, 2015, 28(2):161-70 Pest Manag Sci, 2016, 10.1002/ps.4510 Front Pharmacol, 2018, 9:728	H9c2 cells were incubated with indicated bioactive compounds for 2 hours prior to protein harvest. Cells were lysed and acetyl-lysine (Ac-Lysine), acetyl-histone 3 (Ac-H3 K9/14) and total histone 3 (Total-H3) were assessed via immunoblot. Acetylation of lysine and Ac-H3 (K9/14) increased for gossypol. Acetyl proteins were normalized to total H3 and quantitation performed via Image J software.
S3652	3-Nitropropionic acid 3-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 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.
S8615	Sodium dichloroacetate (DCA) Dichloroacetate, 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 a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.
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).
S8206	Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.	Oncol Rep, 2017, 38(6):3583-3591 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.
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.
S8205	Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.	Drug Des Devel Ther, 2018, 12:1009-1017
S5425	Phenylglyoxal hydrate Phenylglyoxal 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.
S5800^New	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 Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.	Front Immunol, 2013, 4:46 Clin Immunol, 2016, 164:65-77	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 all NK cells (CD3− /CD56+ ) and of the major NK cell subsets deﬁned as CD16+ /CD16− CD56dim and CD56bright were determined by ﬂow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.
S2776	CPI-613 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. Phase 2.
S1247	Leflunomide Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.	J Proteomics, 2012, 79:114-22 Cell Immunol, 2014, 288(1-2):1-7 Toxicol Lett, 2018, 282:154-165	H1299, H460, A549 cells were treated with leflunomide or teriflunomide at indicated concentrations for 24 h.
S2487	Mycophenolic acid Mycophenolic acid is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation.	J Virol Methods, 2016, 238:13-20 Clin Immunol, 2016, 164:65-77
S7185	AGI-5198 AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.	J BIOL CHEM, 2018, 10.1074/jbc.RA117.001385	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.
S8530^New	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.
S1158	MK-8245 MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. Phase 2.
S1680	Disulfiram Disulfiram is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.	J Proteomics, 2012, 79:114-22 Biofabrication, 2018, 10(4):044102	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 is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.	Cell Mol Life Sci, 2014, 71(9):1723-40 J Mol Endocrinol, 2014, 53(2):175-90 Biol Reprod, 2012, 87(2):35	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.
S4169	Teriflunomide Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.	Toxicol Lett, 2018, 282:154-165	Leflunomide or teriflunomide were incubated with H1299, H460, A549 cells at indicated concentrations for or 2, 4 or 6 days, followed by MTT assay.
S8076	PluriSIn #1 (NSC 14613) PluriSIn #1 is an inhibitor of the stearoyl-coA desaturase 1 (SCD1), which is able to selectively eliminate hPSCs.
S2376	Ammonium Glycyrrhizinate Ammonium Glycyrrhizinate inhibits growth and cytopathology of several unrelated DNA and RNA viruses.
S2055	Gimeracil Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
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.
S5146	3-Methylpyrazole 3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
S4116	Isovaleramide Isovaleramide is an anticonvulsant molecule isolated from Valeriana pavonii, it inhibits the liver alcohol dehydrogenases.
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.
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.
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.
S2289	Daidzin Daidzin, 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 is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Phase 2.
S2295	Emodin Emodin is a purgative resin, 6-methyl-1,3,8-trihydroxyanthraquinone, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica).	Mol Nutr Food Res, 2017, 10.1002/mnfr.201600744 ACS Chem Biol, 2015, 10.1021/cb5009487 Food Chem Toxicol, 2013, 55:363-70	Trypsin inhibition dose-response curves in the absence (black circles) and presence (red triangles) of detergent for (A) emodin.
S2296	Enoxolone Enoxolone is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice.
S2302	Glycyrrhizin (Glycyrrhizic Acid) Glycyrrhizin (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).	DNA Cell Biol, 2017, 36(1):67-76	Western blot analysis of TLR2 and CXCR4 after direct inhibition with glycyrrhizin.
S2303	gossypol-Acetic acid Gossypol Acetate is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.	Pigment Cell Melanoma Res, 2015, 28(2):161-70 Pest Manag Sci, 2016, 10.1002/ps.4510 Front Pharmacol, 2018, 9:728	H9c2 cells were incubated with indicated bioactive compounds for 2 hours prior to protein harvest. Cells were lysed and acetyl-lysine (Ac-Lysine), acetyl-histone 3 (Ac-H3 K9/14) and total histone 3 (Total-H3) were assessed via immunoblot. Acetylation of lysine and Ac-H3 (K9/14) increased for gossypol. Acetyl proteins were normalized to total H3 and quantitation performed via Image J software.
S3652	3-Nitropropionic acid 3-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 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.
S8615	Sodium dichloroacetate (DCA) Dichloroacetate, 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 a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.
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).
S8206	Ivosidenib (AG-120) Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.	Oncol Rep, 2017, 38(6):3583-3591 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.
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.
S8205	Enasidenib (AG-221) Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.	Drug Des Devel Ther, 2018, 12:1009-1017
S5425	Phenylglyoxal hydrate Phenylglyoxal 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.