2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • 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-12475
    Mutant IDH1-IN-1
    		Inhibitor 99.43%
    Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1R132H and IDH1R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research.
    Mutant IDH1-IN-1
  • HY-18767A
    (R,S)-Ivosidenib
    		Control 98.01%
    (R,S)-Ivosidenib ((R,S)-AG-120) is a (R,S)-enantiomer of Ivosidenib (AG-120) with lower activity. Ivosidenib can be used in research on IDH1-mutant cancers.
    (R,S)-Ivosidenib
  • HY-W017463
    trans-3-(3-Pyridyl)acrylic acid
    		Inhibitor 99.87%
    trans-3-(3-Pyridyl) acrylic acid is an unsaturated carboxylic acid and synthetic building block, which serves as a synthetic precursor of 3-(3-pyridyl) propanoic acid. trans-3-(3-Pyridyl) acrylic acid can be used to prepare dual mutant IDH1/NAMPT inhibitors and PGE2 antagonist analogs. In addition, trans-3-(3-Pyridyl) acrylic acid exhibits antiviral activity against tobacco mosaic virus (TMV).
    trans-3-(3-Pyridyl)acrylic acid
  • 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-19208
    ZD-2767P
    		Inhibitor
    ZD-2767P (Compound 1) is a reversible and competitive inhibitor of IDH1, with its IC50 value being 410 nM.
    ZD-2767P
  • HY-128888B
    (S,R)-GSK321
    		Control 98.62%
    (S,R)-GSK321 is the (S,R)-enantiomer of GSK321 (HY-18948). 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. 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. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers.
    (S,R)-GSK321
  • 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-18717
    Mutant IDH1-IN-2
    		Inhibitor 98.50%
    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.
    Mutant IDH1-IN-2
  • HY-131312
    Crelosidenib
    		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.
    Crelosidenib
  • 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-159833
    Ranosidenib
    		Inhibitor
    Ranosidenib is a isocitrate dehydrogenase (IDH) inhibitor with antitumor activity.
    Ranosidenib
  • 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-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-13972
    Mutant IDH1 inhibitor
    		Inhibitor 99.08%
    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
    Mutant IDH1 inhibitor
  • 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-168980
    Lanisidenib
    		Inhibitor
    Lanisidenib is the inhibitor for isocitrate dehydrogenase that exhibits antineoplastic activity.
    Lanisidenib
Art. -Nr. Produktname / Synonyms Application Reactivity
Isocitrate Dehydrogenase (IDH) Isoform Comparison

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