2328074-38-8

EML741 is a histone lysine methyltransferase G9a/GLP inhibitor. It also inhibits DNMT1 with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.

EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated[1].

G9a: 23 nM (IC₅₀); G9a: 1.13 μM (Kd); DNMT1: 3.1 μM (IC₅₀)

[1] Milite, et al. Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. J Med Chem. 2019 Mar 14;62(5):2666-2689. DOI:10.1021/acs.jmedchem.8b02008