JQEZ5 (JQ5, EZ005) is a novel potent, selective, SAM-competitive EZH2 inhibitor with IC50 of 80 nM (inhibition of enzymatic function of PRC2).
JQEZ5 demonstrates acutely reduced level of H3K27me3 without affecting mono- and di-methylation, suppresses the proliferation of EZH2-overexpression H661 and H522 cell lines, more effectively than GSK-126 and GSK-343.
JQEZ5 promotes the regression of EZH2-driven tumors in vivo.
