50405-58-8

TC-E 5008 is a cancer-assocaited mutant isocitrate dehydrogenase inhibitor, which was found to be permeable through the blood-brain barrier.

ChEBI: SYC-435 is a cyclic hydroxamic acid that is 1-hydroxypyridin-2(1H)-one in which the hydrogens at positions 4 and 6 are substituted by methyl and benzyl groups, respectively. It is a potent inhibitor of mutant isocitrate dehydrogenase 1 (Ki values of 190 nM against R132H mutant and 120 nM against R132C mutant). It has a role as an EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor and an antineoplastic agent. It is a member of benzenes, a pyridone and a cyclic hydroxamic acid.

R132H IDH1: 190 nM (Ki); R132C IDH1: 120 nM (Ki); WT IDH1: 12.3 μM (Ki)