mIDH1-IN-2 is a brain-penetrating inhibitor of isocitrate dehydrogenase 1 (IDH1). It demonstrates sub-nanomolar potency against IDH1R132H and R132C, with IC50 values of 80.0 and 58.0 nM, respectively, while showing minimal activity against wild-type IDH1/2. Additionally, mIDH1-IN-2 inhibits PDK1 with an IC50 of 0.61 µM and reduces phosphorylation levels of PDH in a dose-dependent manner. The compound also inhibits cell proliferation, induces S-phase arrest, and promotes apoptosis (apoptosis). mIDH1-IN-2 is applicable in cancer research, including studies on gliomas.
Target-Kategorie:
Isocitrate Dehydrogenase (IDH)|||PDK|||Apoptosis
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