A lysine methyltransferase EZH2 (KMT63) inhibitor. DZNep is a selective inhibitor of trimethylation of lysine 27 on histone H3 (H3K27me3) and lysine 20 on histone H4 (H4K20me3). DZNep treatment of cultured human AML cells induces increased expression of the cell-cycle regulators p21, p27, and FBXO32, leading to cell cycle arrest and apoptosis.