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Dehydrogenase inhibitors

Other Metabolism Related Inhibitors

Transferase DPP Aminopeptidase Procollagen C Proteinase P450 (e.g. CYP17) Phospholipase (e.g. PLA) Factor Xa PDE DHFR Carbonic Anhydrase

Isoform-selective Products

ALDH1A

Cat.No.	Product Name	Information	Product Use Citations	Product Validations
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).	EBioMedicine, 2024, 102:105090 Cancer Res Commun, 2024, 4(3):876-894 Cancer Discov, 2023, 13(1):170-193
S6675	(R)-GNE-140	(R)-GNE-140 is an inhibitory agent for LDHA, LDHB, and LDHC, with IC50 values of 3 nM and 5 nM for LDHA and LDHB, respectively. (R)-GNE-140 is 18 times more potent than its S isomer.	J Clin Invest, 2024, 134(17)e177606 J Mol Cell Biol, 2024, mjae056 J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363
S2776	CPI-613 (Devimistat)	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.	Adv Sci (Weinh), 2025, 12(30):e02146 Microbiol Res, 2025, 293:128070 iScience, 2025, 28(1):111525
S5097	Methotrexate disodium	Methotrexate sodium, an analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis.	Chin Med J (Engl), 2023, 10.1097/CM9.0000000000002816 Pharmaceutics, 2023, 15(2)576 Bioact Mater, 2022, 18:459-470
S1680	Tetraethylthiuram disulfide (Disulfiram)	Disulfiram 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).	Nat Commun, 2025, 16(1):8083 Cell Rep Med, 2025, 6(9):102328 Leukemia, 2025, 39(9):2152-2162
S8205	AG-221 (Enasidenib)	Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.	iScience, 2025, 28(2):111833 iScience, 2024, 27(10):110862 Hematol Oncol, 2024, 42(6):e3316
S8615	Sodium Dichloroacetate (DCA)	DCA (Sodium 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 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.	bioRxiv, 2025, 2025.04.03.647023 bioRxiv, 2025, 2025.08.24.671623 bioRxiv, 2025, 2023.08.11.552890
S1247	Leflunomide	Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of this compound is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). This chemical is also an agonist of the AhR.	Cancer Cell, 2025, 43(4):776-796.e14 J Transl Med, 2025, 23(1):917 J Virol, 2025, 99(2):e0211024
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 Clin Invest, 2025, e190215 Front Cell Dev Biol, 2023, 11:1089945 Cell Death Discov, 2022, 8(1):464
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.	EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2 EBioMedicine, 2024, 102:105090 Cancers -Basel), 2023, 15(19)4772
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