2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Isocitrate Dehydrogenase (IDH)

Isocitrate Dehydrogenase (IDH)

Isocitrate Dehydrogenase (IDH)

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Isocitrate dehydrogenase (IDH), one of the key enzymes in the citric acid cycle, catalyzes the oxidative decarboxylation of isocitrate to alpha-ketoglutarate (α-KG) generating carbon dioxide and NADPH/NADH. IDHs belong to a large ancient family of enzymes that play central roles in energy metabolism, amino acid biosynthesis and vitamin production.

IDH protein family consists of three self-regulating enzymes (IDH1, IDH2, and IDH3). IDH1 and IDH2 are both nicotinamide adenine dinucleotide phosphate (NADP)-dependent enzymes that catalyze the oxidative decarboxylation of isocitrate to alpha-ketoglutarate (α-KG), while producing NADPH either in peroxisomes and the cytosol (IDH1) or in mitochondria (IDH2). IDH3 catalyzes the same reaction in the mitochondria, but in a NAD-dependent fashion. Mutations in IDH1 and IDH2 have been demonstrated in a variety of malignancies. IDH inhibitors have engendered hope in IDH1/2 mutant myeloid malignancies.

Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

Isocitrate Dehydrogenase (IDH) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18767
    Ivosidenib
    		Inhibitor 99.85%
    Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
    Ivosidenib
  • HY-18690
    Enasidenib
    		Inhibitor 99.97%
    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.
    Enasidenib
  • HY-104042
    Vorasidenib
    		Inhibitor 99.87%
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
    Vorasidenib
  • HY-15734
    AGI-6780
    		Inhibitor 99.31%
    AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50 of 190±8.1 nM.
    AGI-6780
  • HY-19540
    GSK864
    		Inhibitor 99.93%
    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
    GSK864
  • HY-156158
    IDH2R140Q-IN-2
    		Inhibitor
    IDH2R140Q-IN-2 (compound 36) is an an orally active IDH2R140Q inhibitor (IC50: 29 nM). IDH2R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2R140Q (IC50: 10 nM). IDH2R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2R140Q-IN-2 can be used for research of acute myeloid leukemia (AML).
    IDH2R140Q-IN-2
  • HY-131521
    Oxalomalic acid trisodium
    		Inhibitor
    Oxalomalic acid (Oxalomalate) trisodium is a aconitase and NADP-dependent isocitrate dehydrogenase inhibitor. Oxalomalic acid trisodium inhibits nitrite production and iNOS protein expression in lipopolysaccharide (HY-D1056)-activated J774 macrophages.
    Oxalomalic acid trisodium
  • HY-18082
    AGI-5198
    		Inhibitor 99.77%
    AGI-5198 (IDH-C35) is a potent and selective mutant IDH1R132H inhibitor with an IC50 of 0.07 μM.
    AGI-5198
  • HY-100020
    BAY-1436032
    		Inhibitor 99.48%
    BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
    BAY-1436032
  • HY-18690A
    Enasidenib mesylate
    		Inhibitor 99.85%
    Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
    Enasidenib mesylate
  • HY-114226
    Olutasidenib
    		Inhibitor 99.30%
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
    Olutasidenib
  • HY-104036
    IDH-305
    		Inhibitor 98.75%
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT)).
    IDH-305
  • HY-12475
    Mutant IDH1-IN-1
    		Inhibitor 99.53%
    Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
    Mutant IDH1-IN-1
  • HY-129545
    DS-1001b
    		Inhibitor 99.71%
    DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity.
    DS-1001b
  • HY-18767A
    (R,S)-Ivosidenib
    		Inhibitor 98.12%
    (R,S)-Ivosidenib ((R,S)-AG-120) is the less active enantiomer of Ivosidenib (AG-120).
    (R,S)-Ivosidenib
  • HY-128888B
    (S,R)-GSK321
    		Inhibitor 98.78%
    (S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers.
    (S,R)-GSK321
  • HY-128661
    IDH1 Inhibitor 2
    		Inhibitor 99.40%
    IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.
    IDH1 Inhibitor 2
  • HY-128888
    (R,R)-GSK321
    		Inhibitor 99.31%
    (R,R)-GSK321 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. (R,R)-GSK321 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity.
    (R,R)-GSK321
  • HY-112289
    IDH889
    		Inhibitor 99.96%
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
    IDH889
  • HY-13972
    Mutant IDH1 inhibitor
    		Inhibitor 99.40%
    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
    Mutant IDH1 inhibitor
Cat. No. Product Name / Synonyms Application Reactivity
Isocitrate Dehydrogenase (IDH) Isoform Comparison

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