CPI-360 is a potent, selective EZH2 inhibitor with IC50 of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively. CPI-360 decreases cellular levels of H3K27me3 and H3K27me2 (EC50, 56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin's lymphoma (NHL) cell lines. CPI-360 (200 mg/kg) reduced tumor growth of KARPAS-422 xenografts in mice.
