MS8511 是一种选择性的G9a/GLP共价的不可逆抑制剂，可靶向底物结合位点的半胱氨酸残基，IC50值为 100 nM ( G9a) 和 140 nM (GLP)，Kd值44 nM (G9a) 和 46 nM (GLP)。 MS8511 可降低细胞内 H3K9me2 水平并提高抗增殖活性。MS8511 可用于研究多种癌症 (包括脑癌、乳腺癌、卵巢癌、肺癌、膀胱癌、黑色素瘤、结肠直肠癌) 和其他疾病,如阿尔茨海默病 (AD)、镰状细胞病、Prader-Willi 综合征 (PWS).

MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC 50 values of 100 nM (G9a) and 140 nM (GLP), and K d 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) [1].

MS8511 (Compound 8, 0-100 μΜ, 10 min) selectively inhibits G9a and GLP against other PKMTs and PRMTs, with IC 50 values of 100 nM (G9a) and 140 nM (GLP) [1]. MS8511 (50 min) prefers covalent modification for G9a over GLP, with K d 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]. Western Blot Analysis [1] Cell Line: MDA-MB-231, K562 cells. Concentration: 0.2, 1, 5 μM. Incubation Time: 24, 48, 72 h. Result: Reduced the H3K9me2 mark in a concentration- and time-dependent manner. Cell Viability Assay [1] Cell Line: MDA-MB-231 cells Concentration: 0.8, 1.6, 3.1 6.3, 12.5, 25 μM. Incubation Time: 3 days Result: Inhibited the growth of MDA-MB-231 cells.

C28H41N5O3

495.66

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years