MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
MS8511 (Compound 8, 0-100 μΜ, 10 min) selectively inhibits G9a and GLP against other PKMTs and PRMTs, with IC50 values of 100 nM (G9a) and 140 nM (GLP)[1].
MS8511 (50 min) prefers covalent modification for G9a over GLP, with Kd values of 44 nM (G9a) and 46 nM (GLP)[1].
MS8511 (0-5 μM, 24-72 h) effectively reduces the H3K9me2 mark in MDA-MB-231 and K562 cellssup>[1].
MS8511 (0.8-25 μM, 3 days) inhibits the growth of MDA-MB-231 cells[1].
References:
[1]. Kwang-Su Park, et al. Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J Med Chem. 2022 Jun 28.