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-131312
    LY3410738
    		Inhibitor
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (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 mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
    LY3410738
  • HY-150238
    IDH1 Inhibitor 7
    		Inhibitor 99.46%
    IDH1 Inhibitor 7 (Compound 88) is an IDH1 inhibitor with an IC50 of less than 100 nM.
    IDH1 Inhibitor 7
  • HY-112601
    IDH1 Inhibitor 1
    		Inhibitor 99.96%
    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity.
    IDH1 Inhibitor 1
  • HY-P2993
    Isocitrate dehydrogenase, Porcine heart
    Isocitrate dehydrogenase, Porcine heart (ICDH) is a citric acid or tricarboxylic acid cycle enzyme, is often used in biochemical studies. Isocitrate dehydrogenase catalyzes the oxidative decarboxylation of isocitrate to α-ketoglutarate and reduces NAD(P)+ to NAD(P)H, it plays important roles in cellular metabolism.
    Isocitrate dehydrogenase, Porcine heart
  • HY-150238S
    IDH1 Inhibitor 7-d2
    		Inhibitor 99.93%
    IDH1 Inhibitor 7-d2 is the deuterium labeled IDH1 Inhibitor 7 (HY-150238). IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC50 of less than 100 nM.
    IDH1 Inhibitor 7-d<sub>2</sub>
  • HY-41648
    IDH1 Inhibitor 8
    		Inhibitor ≥99.0%
    IDH1 Inhibitor 8 (91) is isocitrate dehydrogenase 1 (IDH1) inhibitor. IDH1 Inhibitor 8 can be used for the research of cancer.
    IDH1 Inhibitor 8
  • HY-145594
    Safusidenib
    		Inhibitor
    Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.
    Safusidenib
  • HY-107977
    IDH1 Inhibitor 3
    		Inhibitor
    IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H.
    IDH1 Inhibitor 3
  • HY-110144
    TC-E 5008
    		Inhibitor
    TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines.
    TC-E 5008
  • HY-128888A
    (S,S)-GSK321
    		Inhibitor 99.78%
    (S,S)-GSK321 is a (S,S)-enantiomer of GSK321.
    (S,S)-GSK321
  • HY-114459
    Mutant IDH1-IN-4
    		Inhibitor ≥99.0%
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
    Mutant IDH1-IN-4
  • HY-112289B
    (1R)-IDH889
    (1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. 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.
    (1R)-IDH889
  • HY-143306
    IDH1 Inhibitor 5
    		Inhibitor
    IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively.
    IDH1 Inhibitor 5
  • 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-146002
    IDH2R140Q-IN-1
    		Inhibitor
    IDH2R140Q-IN-1 (compound C6) is a potent inhibitor of IDH2R140Q, with an IC50 of 6.1 nM. IDH2R140Q-IN-1 can be used for the research of acute myeloid leukemia.
    IDH2R140Q-IN-1
  • HY-149359
    IHMT-IDH1-053
    		Inhibitor
    IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants.
    IHMT-IDH1-053
  • HY-136686
    IDH-C227
    		Inhibitor
    IDH-C227 is a potent and selective IDH1R132H inhibitor. IDH-C227 has anticancer effcts.
    IDH-C227
  • HY-143234
    mIDH1-IN-1
    		Inhibitor
    mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research.
    mIDH1-IN-1
  • HY-N12390
    Alternaphenol B2
    		Inhibitor
    Alternaphenol B2 is a selective IDH1 inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC50 values of 41.9 μM.
    Alternaphenol B2
  • HY-121736
    AGI-12026
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma.
    AGI-12026
Cat. No. Product Name / Synonyms Application Reactivity
Isocitrate Dehydrogenase (IDH) Isoform Comparison

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