CM-579 trihydrochloride 是一线的、可逆的，G9a 和DNA 甲基转移酶 (DNMT) 的双抑制剂，其IC50 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。
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)
The Kd of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC50s of 92 nM and 1000 nM, respectively[1].
[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.
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