CPI-1205

CPI-1205 is a highly potent (biochemical IC₅₀ = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of the histone lysine methyltransferase EZH2 (biochemical IC₅₀ = 0.002 μM, cellular EC₅₀ = 0.032 μM). Upon oral administration, CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2.