Isocitrate Dehydrogenase (IDH)
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
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Isocitrate Dehydrogenase (IDH) Related Products (75)
Related Products (75)
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Antibodies (3)
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Isocitrate Dehydrogenase (IDH) Isoform Comparison
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Mutant IDH1-IN-1
0 ImagesSynonyms: Agios 135Mutant 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.
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(R,S)-Ivosidenib
0 ImagesSynonyms: (R,S)-AG-120(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.
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trans-3-(3-Pyridyl)acrylic acid
0 Imagestrans-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).
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Isocitrate dehydrogenase, Porcine heart
0 ImagesIsocitrate 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.
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IDH889
0 ImagesIDH889 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.
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ZD-2767P
0 ImagesCat. No.: HY-19208CAS No.: 156079-88-8ZD-2767P (Compound 1) is a reversible and competitive inhibitor of IDH1, with its IC50 value being 410 nM.
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(S,R)-GSK321
0 Images(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.
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Mutant IDH1-IN-2
0 ImagesMutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
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Crelosidenib
0 ImagesCat. No.: HY-131312CAS No.: 2230263-60-0Synonyms: LY3410738; Mutant IDH1-IN-6Mutant 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.
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IDH1 Inhibitor 1
0 ImagesIDH1 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.
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IDH1 Inhibitor 7
0 ImagesIDH1 Inhibitor 7 (Compound 88) is an IDH1 inhibitor with an IC50 of less than 100 nM.
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IDH1 Inhibitor 7-d2
0 ImagesIDH1 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.
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Mutant IDH1 inhibitor
0 ImagesMutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
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IDH1 Inhibitor 3
0 ImagesCat. No.: HY-107977CAS No.: 2171081-24-4IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H.
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TC-E 5008
0 ImagesCat. No.: HY-110144CAS No.: 50405-58-8TC-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.
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(S,S)-GSK321
0 Images(S,S)-GSK321 is a (S,S)-enantiomer of GSK321.
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Mutant IDH1-IN-4
0 ImagesMutant 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.
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Lanisidenib
0 ImagesCat. No.: HY-168980CAS No.: 2135537-20-9Lanisidenib is the inhibitor for isocitrate dehydrogenase that exhibits antineoplastic activity.
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(1R)-IDH889
0 Images(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.
