2089617-83-2

MS012 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. MS012 exhibited stronger binding affinity to GLP (Kd = 46 ± 15 nM) than G9a (Kd = 610 ± 68 nM). MS012 was 13-fold selective for GLP over G9a. G9a-like protein (GLP) and G9a are highly homologous protein lysine methyltransferases (PKMTs) sharing approximately 80% sequence identity in their catalytic domains. GLP and G9a form a heterodimer complex and catalyze mono- and dimethylation of histone H3 lysine 9 and nonhistone substrates.

MS012 is a selective GLP inhibitor (IC50=7 nM). MS012 can be used in research of GLP dysregulation, including cancer, inflammatory diseases, and neuroregenerative disorders[1].

[1] Xiong Y, et al. Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J Med Chem. 2017 Mar 9;60(5):1876-1891. DOI:10.1021/acs.jmedchem.6b01645