MS8511

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MS8511

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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)，K_d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).

生物活性

MS8511 is a selectiveG9a/GLPcovalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, withIC₅₀values of 100 nM (G9a) and 140 nM (GLP), andK_dvalues 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, colorectalcancer, andother diseasesuch as Alzheimer’s disease (AD), sickle cell disease, Prader–Willi syndrome (PWS)^[1].

IC₅₀& Target

G9a

100 nM (IC₅₀)

G9a

44 nM (Kd)

GLP

140 nM (IC₅₀)

GLP

46 nM (Kd)

体外研究
(In Vitro)

MS8511 (Compound 8, 0-100 μΜ, 10 min) selectively inhibits G9a and GLP against other PKMTs and PRMTs, with IC₅₀values of 100 nM (G9a) and 140 nM (GLP)^[1].
MS8511 (50 min) prefers covalent modification for G9a over GLP, with K_dvalues 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.

分子量

495.66

Formula

C₂₈H₄₁N₅O₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.