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.
