EZH2-IN-23 (Compound 25) is an EZH2 inhibitor that exhibits potent enzymatic inhibition of the PRC2 complex ( EZH2 , EED, SUZ12, AEBP2, RbAp48) with a biochemical IC 50 of 0.8 nM. EZH2-IN-23 inhibits H3K27 trimethylation in cellular assays, showing an IC 50 of 40 nM. EZH2-IN-23 displays good rat PKproperties with 100 % oral bioavailability.
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