Dehydrogenase

Inhibitory Selectivity

Isoform-specific Inhibitors

Dehydrogenase Products

New Dehydrogenase Products
Catalog No. Information Product Use Citations Product Validations
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.

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).

S2987New

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.

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).

S9776New

AG-636

AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.

S4929New

Enasidenib Mesylate

Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

S3565New

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.

S3574New

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.

S9783New

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.

S9721New

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.

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.

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.

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.

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.

S7241

AGI-6780

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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 (ALDH2*1) and ALDH2*2.

Catalog No. Information Product Use Citations Product Validations
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.

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).

S2987New

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.

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).

S9776New

AG-636

AG-636 is an orally available inhibitor of dihydroorotate dehydrogenase (DHODH) with potential antineoplastic activity.

S4929New

Enasidenib Mesylate

Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

S3565New

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.

S3574New

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.

S9783New

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.

S9721New

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.

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.

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.

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.

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.

S7241

AGI-6780

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

S6626

Brequinar (DUP785)

Brequinar (DUP785, NSC 368390) is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.

Catalog No. Information Product Use Citations Product Validations
S5800

Alda 1

Alda 1 is an ALDH2 agonist that activates catalysis for both wild-type ALDH2 (ALDH2*1) and ALDH2*2.