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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.

FilterSignaling PathwaysMetabolismIsocitrate Dehydrogenase (IDH)
  • Mutant IDH1-IN-2
    T121281429176-69-1In house
    Mutant IDH1-IN-2 is a mutant Isocitrate dehydrogenase (IDH) proteins inhibitor
    • $97
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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
  • Mutant IDH1-IN-1
    T20431355326-21-4
    Mutant IDH1-IN-1 is a potent mutant IDH1 R132 h inhibitor with IC50 < 0.1 uM.
    • $64
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  • Alternaphenol B2
    T83133
    Alternaphenol B2, a selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1m), is sourced from the coral-derived fungus Parengyodontium album SCSIO SX7W11. It exhibits inhibitory activity specifically against the IDH1 R132H mutation, with an IC50 of 41.9 μM [1].
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  • IHMT-IDH1-053
    T78758
    IHMT-IDH1-053 (compound 16) is an irreversible inhibitor exhibiting high selectivity for the IDH1 R132H mutant, achieving an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, both wild-type and mutants. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 value of 28 nM. The compound engages with the R132H protein at an allosteric site near the NAPDH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 impedes the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].
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  • 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).
    • $70
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  • Ivosidenib
    T36171448347-49-6
    Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2 hG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells.
    • $42
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  • AGI-5198
    T21041355326-35-0
    AGI-5198 (IDH-C35) is a highly effective and specific inhibitor of IDH1 R132H/R132C mutants (IC50: 0.07/0.16 μM).
    • $32
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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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  • DS-1001b
    T77411898207-64-1
    DS-1001b is an inhibitor of mutant IDH-1 (Isocitrate Dehydrogenase-1)
    • $31
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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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  • 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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  • Mutant IDH1 inhibitor
    T161611429180-08-4
    Mutant IDH1 inhibitor is an effective inhibitor of mutant IDH1 R132H (IC50: < 72 nM).
    • $58
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