MIDH1-IN-2

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.