Isocitrate dehydrogenase (IDH), a crucial enzyme in the citric acid cycle, catalyzes the oxidative decarboxylation of isocitrate to alpha-ketoglutarate (-KG), which produces carbon dioxide and NADPH/NADH. IDHs are members of a large, long-extinct family of enzymes that are essential for producing vitamins, amino acids, and energy.
Three self-regulating enzymes (IDH1, IDH2, and IDH3) make up the IDH protein family. IDH1 and IDH2 are nicotinamide adenine dinucleotide phosphate (NADP)-dependent enzymes that produce NADPH either in peroxisomes and the cytosol (IDH1) or in mitochondria (IDH2). They both catalyze the oxidative decarboxylation of isocitrate to alpha-ketoglutarate (-KG). In the mitochondria, IDH3 also catalyzes the same reaction, but it does so in a NAD-dependent manner. Numerous malignancies have been shown to harbor IDH1 and IDH2 mutations. IDH inhibitors have raised hope for myeloid cancers with IDH1/2 mutations.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74039 | (1R)-IDH889 | 1429179-08-7 | (1R)-IDH889 is the inactive isomer of IDH889 and could be utilized as a control compound in experiments. |
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V74044 | (R,R)-GSK321 | 1816272-19-1 | (R,R)-GSK321 is an inhibitor (blocker/antagonist) of wild-type isocitrate dehydrogenase 1 (WT IDH1) with IC50 of 120 nM. |
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V74037 | (R,S)-Ivosidenib ((R,S)-AG-120) | 2070009-31-1 | (R,S)-Ivosidenib ((R,S)-AG-120) is the less active enantiomer of Ivosidenib (AG-120). |
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V74042 | (S,S)-GSK321 | 1816272-20-4 | (S,S)-GSK321 is the (S,S)-enantiomer of GSK321. |
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V80423 | Alternaphenol B2 | IDH1 Inhibitor | |
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V34666 | DS-1001B | 1898207-64-1 | DS-1001B is a potent and selective mutant IDH1(Isocitrate Dehydrogenase-1) inhibitor with antitumor activity, ameliorating aberrant histone modifications and impairing tumor activity in chondrosarcoma. |
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V3408 | Enasidenib mesylate | 1650550-25-6 | Enasidenib mesylate (formerly known as AG-221; CC-90007;AG221; CC90007; trade name Idhifa), the mesylate salt of enasidenib, is a first-in-class, oral, potent and selective IDH2 (Isocitrate dehydrogenase 2)inhibitorapproved in 2017 for the treatment of relapsed or refractory acute myeloid leukemia in people with specific mutations of the IDH2 gene, determined by an FDA-approved IDH2 companion diagnostic test. |
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V3599 | GSK864 | 1816331-66-4 | GSK864 is a novel, potent and selective isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G withIC50values of 8.8, 15.2 and 16.6 nM. |
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V74043 | IDH-C227 | 1355324-14-9 | IDH-C227 is a potent and specific IDH1R132H inhibitor. |
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V74047 | IDH1 Inhibitor 7 | 2135309-56-5 | IDH1 Inhibitor 7 (Compound 88) is an IDH1 inhibitor (antagonist) with IC50 less than 100 nM. |
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V74041 | IDH1 Inhibitor 7-d2 | 2135309-51-0 | IDH1 Inhibitor 7-d2 is the deuterated form of IDH1 Inhibitor 7. |
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V74038 | IDH2R140Q-IN-2 | 2749568-16-7 | IDH2R140Q-IN-2 (Compound 36) is an orally bioactive IDH2R140Q inhibitor (IC50= 29 nM). |
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V78813 | IHMT-IDH1-053 | IHMT-IDH1-053 (compound 16) is a selective and irreversible inhibitor of IDH1 mutations with IC50 of 4.7 nM for IDH1 R132H. | |
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V74040 | Isocitrate dehydrogenase (ICDH) | 9028-48-2 | Isocitrate dehydrogenase (ICDH) Isocitrate dehydrogenase is a citric acid or tricarboxylic acid cycle enzyme widely used in biochemical research. |
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V3884 | Ivosidenib | 1448347-49-6 | Ivosidenib(formerly known as AG-120 or RG-120; trade name: Tibsovo®) is a novel, small molecule, orally bioavailable inhibitor of mutated cytosolic isocitrate dehydrogenase 1 (IDH1) developed by Agios Pharmaceuticals and has been approved for the treatment of cancer in patients with IDH1 mutations. |
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V74045 | LY3410738 (Mutant IDH1-IN-6) | 2230263-60-0 | Mutant IDH1-IN-6 is a specific and orally bioactive mutant IDH inhibitor (antagonist) with IC50s of 6.27 nM, 3.71 nM and 36.9 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes respectively. |
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V3432 | Mutant IDH1-IN-1 | 1355326-21-4 | Mutant IDH1-IN-1 is a novel, potent and mutant-selectiveIDH1 (isocitrate dehydrogenase 1)inhibitor with withIC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively. |
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V74046 | Safusidenib (AB-291; DS-1001) | 1898206-17-1 | Safusidenib (AB-291; DS-1001) is an orally bioavailable and selective IDH1 mutant inhibitor. |
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