EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC 50 of 23 nM, K d of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC 50 , 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.