EED226 is a polycomb repressive complex 2 ( PRC2 ) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development ( EED ) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC 50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
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