EED-226 (2083627-02-3) is a potent (IC50 = 23.4 nM) and selective allosteric inhibitor of the EED subunit of the methyltransferase polycomb repressive complex 2 (PRC2).1,2 It caused drastic proliferation inhibition in lymphoma cells with EZH2 mutations and caused shrinkage and slower tumor growth in mice using a subcutaneous xenograft model of Karpas422.
1) Huang et al. (2017), Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy; J. Med. Chem. 60 2215
2) Qi et al. (2017), An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED; Nat. Chem. Biol. 13 381