Potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor (IC50 = 11 nM). Selectively binds EZH2 over a panel of 22 methyltransferases. Reduces global level of the PRC2-associated mark H3K27me3 in K562 cells. Suppresses cell growth in CML cells. Inhibits colony formation of primary human CD34+ CML stem/ progenitor cells. Antitumor effects in vivo. Purity 98%. MW (observed): 542.69