931078-17-0

CPI-905 is a potent and selective EZH2 inhibitor (IC50 = 39.5 nM). The histone lysine methyltransferase (MT) Enhancer of Zeste Homolog 2 (EZH2) is considered an oncogenic driver in a subset of germinal center B-celllike diffuse large B cell lymphoma (GCB-DLBCL) and follicular lymphoma due to the presence of recurrent, monoallelic mutations in the EZH2 catalytic domain. .

CPI-905 is a potent, selective, and cell-active EZH2 inhibitor[1].

[1] William D Bradley, et al. EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation. Chem Biol. 2014 Nov 20;21(11):1463-75. DOI:10.1016/j.chembiol.2014.09.017