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. References: Xiong Y, Li F, Babault N, Dong A, Zeng H, Wu H, Chen X, Arrowsmith CH, Brown PJ, Liu J, Vedadi M, Jin J. Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J Med Chem. 2017 Feb 14. doi: 10.1021/acs.jmedchem.6b01645. [Epub ahead of print] PubMed PMID: 28135087.

纯度：≥98%

CAS：2089617-83-2