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 (76)
Related Products (76)
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Antibodies (3)
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Isocitrate Dehydrogenase (IDH) Isoform Comparison
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SH1573
0 ImagesCat. No.: HY-164526CAS No.: 2376068-96-9SH1573 is an orally active mIDH2 inhibitor. SH1573 has a strong and selective inhibitory effect on mIDH2 R140Q protein (IC50=4.78 nmol/L), and can effectively reduce the production of the carcinogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum and tumors. SH1573 can be used for the study of acute myeloid leukemia (AML).
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Mutant IDH1-IN-7
0 ImagesCat. No.: HY-175213Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells.
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BRD2879
0 ImagesCat. No.: HY-120765CAS No.: 1304750-47-7BRD2879 is a potent IDH1-R132H inhibitor with IC50 values of 0.05, 2.5, >20, >20 µM for IDH1-R132H, IDH1-R132C, IDH1-WT, IDH2-R140Q, respectively. BRD2879 reduces (R)-2-hydroxyglutarate (R-2HG) levels.
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AGI-14100
0 ImagesCat. No.: HY-120181CAS No.: 1448346-43-7AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors.
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Ivosidenib (Standard)
0 ImagesCat. No.: HY-18767RCAS No.: 1448347-49-6Synonyms: AG-120 (Standard)Ivosidenib (Standard) is the analytical standard of Ivosidenib (HY-18767). This product is intended for research and analytical applications. 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.
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DA-11004
0 ImagesCat. No.: HY-16164CAS No.: 57404-51-0DA-11004 is an orally active NADP-dependent isocitrate dehydrogenase (IDPc) inhibitor with an IC50 of 1.49 μM. DA-11004 reduces NADPH production, decreases plasma NADPH levels and plasma free fatty acid levels. DA-11004 lowers plasma glucose levels, inhibits fatty acid synthesis in adipose tissue, reduces weight gain and decreases epididymal and retroperitoneal fat content. DA-11004 exerts antidiabetic effects in mice fed a high-fat and high-sugar diet. DA-11004 can be used for research on obesity and type 2 diabetes.
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IDH1 Inhibitor 9
0 ImagesCat. No.: HY-162631CAS No.: 3037967-71-5IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity.
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mIDH1-IN-2
0 ImagesCat. No.: HY-175770mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma.
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Vorasidenib (Standard)
0 ImagesSynonyms: AG-881 (Standard)Vorasidenib (Standard) is the analytical standard of Vorasidenib (HY-104042). This product is intended for research and analytical applications. 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 can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation.
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Mutant IDH1-IN-3
0 ImagesCat. No.: HY-100476CAS No.: 1648909-73-2Mutant IDH1-IN-3 (Compound 1) is a selective allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). Mutant IDH1-IN-3 has an IC50 of 13 nM for R132H IDH1. Mutant IDH1-IN-3 inhibits the production of D-2-hydroxyglutaric acid (2HG) in cells. Mutant IDH1-IN-3 can be used in the study of cancer.
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Alternaphenol B2
0 ImagesCat. No.: HY-N12390Alternaphenol 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.
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Enasidenib (Standard)
0 ImagesSynonyms: AG-221 (Standard)
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Enasidenib mesylate (Standard)
0 ImagesCat. No.: HY-18690ARCAS No.: 1650550-25-6Synonyms: AG-221 mesylate (Standard)
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BAY-1436032 (Standard)
0 ImagesCat. No.: HY-100020RCAS No.: 1803274-65-8BAY-1436032 (Standard) is the analytical standard of BAY-1436032 (HY-100020). This product is intended for research and analytical applications. BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
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Crelosidenib gentisate
0 ImagesCat. No.: HY-131312ACAS No.: 2759438-85-0Synonyms: LY3410738 gentisate; Mutant IDH1-IN-6 gentisateCrelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 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. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes.
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AGI-12026
0 ImagesCat. No.: HY-121736CAS No.: 1446501-77-4Synonyms: AGI-026
