Description
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).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.
Uses
EED 226 is a potent, selective and orally bioavailable EED inhibitor, inducing robust and sustained tumor regression in specific models. Effective PRC2 inhibitorin the treatment of PRC2-dependant cancers.
References
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
