CPI-455 hydrochloride

CPI-455 hydrochloride is a potent and selective inhibitor of KDM5 demethylases. which reduces survival of drug-tolerant cancer cells. CPI-455 binds to the demethylase active site and selectively inhibits KDM5A-D (IC50s = 2-10 nM) over KDM2-4, 6, and 7 family members (IC50s = 1 to >25 μM). It increases histone H3K4me2/3 methylation in vitro and decreases the number of drug-tolerant cells in PC9 non-small cell lung, M14 melanoma, and SKBR3 breast cancer cell populations.