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IHMT-IDH1-053

Catalog No. T78758

IHMT-IDH1-053 (compound 16) is an irreversible inhibitor exhibiting high selectivity for the IDH1 R132H mutant, achieving an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, both wild-type and mutants. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 value of 28 nM. The compound engages with the R132H protein at an allosteric site near the NAPDH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 impedes the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].

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IHMT-IDH1-053, CAS N/A

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Biological Description

Chemical Properties

Storage & Solubility Information

Description

Targets&IC50

R132H IDH1:4.7 μM

Molecular Weight	532.63
Formula	C25H33FN6O4S

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IHMT-IDH1-053 Metabolism Isocitrate Dehydrogenase (IDH) inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.