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TargetMol | Tags Metabolism
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Isocitrate Dehydrogenase (IDH)

Isocitrate dehydrogenase (IDH) and is an enzyme that catalyzes the oxidative decarboxylation of isocitrate, producing alpha-ketoglutarate (α-ketoglutarate) and CO2. This is a two-step process, which involves oxidation of isocitrate (a secondary alcohol) to oxalosuccinate (a ketone), followed by the decarboxylation of the carboxyl group beta to the ketone, forming alpha-ketoglutarate. In humans, IDH exists in three isoforms: IDH3 catalyzes the third step of the citric acid cycle while converting NAD+ to NADH in the mitochondria. The isoforms IDH1 and IDH2 catalyze the same reaction outside the context of the citric acid cycle and use NADP+ as a cofactor instead of NAD+. They localize to the cytosol as well as the mitochondrion and peroxisome.

FilterHomeSignaling PathwaysMetabolismIsocitrate Dehydrogenase (IDH)
Ivosidenib
T36171448347-49-6
Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.
  • $42
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TargetMol | Inhibitor Hot
DS-1001b
T77411898207-64-1
DS-1001b is an inhibitor of mutant IDH-1 (Isocitrate Dehydrogenase-1)
  • $31
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Vorasidenib
T73071644545-52-7
Vorasidenib (PVM MA) is an inhibitor of mutant isocitrate dehydrogenase (IDH; IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively)
  • $48
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Enasidenib
T23461446502-11-9
Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity.
  • $39
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Mutant IDH1-IN-2
T121281429176-69-1In house
Mutant IDH1-IN-2 is an inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with an IC50 of 16.6 nM in fluorescence biochemical assay and an IC50 of <22 nM in LS-MS biochemical assay.
  • $58
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AGI-026
T265751446501-77-4
AGI-026 (AGI-12026) is a novel and potent dual inhibitor of the mutant isocitrate dehydrogenase mIDH1/2 with the advantages of oral administration and penetration of the blood-brain barrier, with a drug concentration to plasma concentration ratio (brain/plasma ratio) of 1.5 in brain tissue, and the ability to reduce the accumulation of the carcinogenic metabolite d-2-hydroxyglutarate (2-HG), which is used in the study of mIDH gliomas.
  • $293
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IDH2R140Q-IN-2
T797452749568-16-7In house
IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).
  • $397 TargetMol
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Crelosidenib
T397162230263-60-0
Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme.
  • $397
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IDH889
T155511429179-07-6
IDH889 is a brain penetrant, an allosteric and mutant specific IDH1 inhibitor. IDH889 has effective selectivity for IDH1 R132* mutations (IC50s: 0.02 μM, 0.072 μM, and 1.38 μM for IDH1R132H, IDH1R132C, and IDH1wt).
  • $105
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AGI-14100
T250061448346-43-7In house
AGI-14100 is a novel and orally available mIDH1 inhibitor.AGI-14100 is used for the treatment of primary human myeloid leukemia.
  • $147
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GSK321
T320091816331-63-1
GSK321 is a selective and potent mutant isocitrate dehydrogenase 1 (IDH1) inhibitor that inhibits lipid synthesis and blocks cell proliferation in OPA1-deficient MEFs and prevents cytoplasmic glutamine reductive carboxylation.GSK321 has been used in the study of leukemia.
  • $149
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AG-120 (racemic)
T222531448346-63-1
AG-120 (racemic), the racemic mixture of AG-120, is an orally available isocitrate dehydrogenase type 1 (IDH1) inhibitor, and shows potential antineoplastic activity.
  • $40
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AGI-6780
T18091432660-47-3
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.
  • $31
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TargetMol | Citations Cited
BAY-1436032
TQ00421803274-65-8
BAY-1436032 is a novel, selective and orally available inhibitor of pan-mutant isocitrate dehydrogenase 1 (IDH1).
  • $31
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TargetMol | Inhibitor Hot
IDH-305
T155501628805-46-8
IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.
  • $52
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Enasidenib mesylate
T2346L1650550-25-6
Enasidenib mesylate (AG-221 mesylate) is a potent and selective IDH2 mutase inhibitor that promotes differentiation of leukemia myeloid cells for the treatment of acute myeloid leukemia.
  • $40
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GSK864
T154421816331-66-4
GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.
  • $68
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TargetMol | Inhibitor Hot
Olutasidenib
T163841887014-12-1
Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively).
  • $56
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AGI-5198
T21041355326-35-0
AGI-5198 (IDH-C35) is a potent and selective inhibitor of IDH1 R132H and R132C mutants, with IC50 values of 0.07 μM and 0.16 μM, respectively.
  • $31
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Mutant IDH1 inhibitor
T161611429180-08-4
Mutant IDH1 inhibitor is an effective inhibitor of mutant IDH1 R132H (IC50: < 72 nM).
  • $35
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Mutant IDH1-IN-1
T20431355326-21-4
Mutant IDH1-IN-1 is a potent inhibitor of the mutant IDH1 R132 h, exhibiting an IC50 of less than 0.1 μM.
  • $39
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IHMT-IDH1-053
T78758
IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].
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(R,S)-Ivosidenib
T134382070009-31-1
(R,S)-Ivosidenib is the less active enantiomer of Ivosidenib .
  • $398
5 days
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IDH1 Inhibitor 2
T116112244895-42-7
IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor through direct covalent modification of His315, with an IC50 of 110 nM.
  • $4,120
8-10 weeks
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