|Product Name||EPZ6438||CAS No.||1403254-99-8|
|Molecular Weight||572.73756||Molecular Formula||C34H44N4O4|
EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with Ki of 2.5±0.5 nM.
EPZ-6438 inhibits EZH2 in a manner competitive with the substrate S-adenosylmethionine (SAM). EPZ-6438 inhibits EZH1, EZH2(in peptide assay), EZH2 (in nucleosome assay) with IC50of 392 nM, 11 nM and 16 nM, respectively. EPZ-6438 displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs tested.