ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM.
ATR-101 induces H295R cell apoptosis, causes mitochondrial hyperpolarization, reactive oxygen release, and ATP depletion, caspase-3/7 activation, and membrane permeabilization.
ATR-101 decreases the formation of cholesteryl esters and increases FC levels in H295R adrenocortical carcinoma cells.
ATR-101 inhibits the establishment and impeds the growth of ACC-derived H295R cell xenografts in mice; orally active.
