2448471-08-5

CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells[1].

DNA Methyltransferase: 32 nM (IC₅₀); DNMT1: 1.5 nM (Kd); DNMT3A: 92 nM (IC₅₀); DNMT3B: 1000 nM (IC₅₀); G9a: 16 nM (IC₅₀)

[1] San José-Enériz E, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424. DOI:10.1038/ncomms15424