1197196-63-6

MS0124 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. MS0124 was 34-fold more selective for GLP (IC50 =_x000D_ 13 ± 4 nM) over G9a (IC50 = 440 ± 63 nM). 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

MS0124 is a potent selective G9a-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM for GLP and G9a,respectively[1].

[1] Yan Xiong, et al. Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg Med Chem DOI:10.1016/j.bmc.2017.06.021