Description: EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM. Target: Histone Methyltransferase. Smiles: N(CC1=CC=CO1)C=2N3C(C(=CN2)C4=CC=C(S(C)(=O)=O)C=C4)=NN=C3. References: Qi W, et al. Nat Chem Biol. 2017, 13(4):381-388.

EED226 is a potent and allosteric inhibitor of the histone H3K27me3 methyltransferase activity of polycomb repressive complex 2 (PRC2, IC50 = 23.4 nM in an enzyme assay with H3K27me0 peptide as the substrate). It exhibits dose-dependent displacement of H3K27me3 binding to the EED subunit of PCR2 but has no effect on...