EED226 (EED 226) is a potent, selective, orally bioavailable PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED (IC50=22 nM).
EED226 shows remarkable selectivity over 21 other PRMTs, with one exception EZH1.
EED226 potently reduces global H3K27Me3 mark in cells and demonstrates selectively cell killing effects in cells carrying a heterozygous Y641N mutation.
EED226 induces robust and sustained tumor regression in EZH2MUT pre-clinical DLBCL model.
