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Results for "

idh1wt

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  • Inhibitors & Agonists
    4
    TargetMol | Inhibitors_Agonists
IDH1 Inhibitor 1
T116132234285-81-3
IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).
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10-14 weeks
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IDH-305
T155501628805-46-8
IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.
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TargetMol | Inhibitor Sale
IDH889
T155511429179-07-6
IDH889 is a brain penetrant, an allosteric and mutant specific IDH1 inhibitor. IDH889 has effective selectivity for IDH1 R132* mutations (IC50s: 0.02 μM, 0.072 μM, and 1.38 μM for IDH1R132H, IDH1R132C, and IDH1wt).
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6-8 weeks
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IHMT-IDH1-053
T78758
IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].
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