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CAS No.: 1831110-54-3

MS023 Catalog No. CSN18048

Synonyms: MS023

MS023 is a potent and selective chemical probe for Type I PRMTs with IC50 values of 30, 119, 83, 8, and 8 nM for PRMTs 1,3,4,6,and 8, respectively. MS023 is active in cells.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 values of 30, 119, 83, 4 and 5nM for PRMT1, 3, 4, 6 and 8, respectively. MS023 inhibited both PRMT1 methyltransferase activity shown by decreased level of H4R3me2a post 48h in MCF7 cells, and PRMT6 methyltransferase activity shown by decreased level of H4R3me2a post 20h in HEK293 cells at concentration>37nM. Treatment with MS023 at 10μM or 50μM for 2 days led a significant decrease in global levels of arginine asymmetric dimethylation (Rme2a) and a concurrent increase in global levels of arginine monomethylation (Rme1) and arginine symmetric demethylation in MCF7 and HEK293 cells^[2].
作用机制MS023 can effectively occupy the arginine side chain binding pocket of the substrate and likely form the substrate-inhibitor-PRMT6 complex without significant penalty of free energy.^[2]
动物研究
剂量
Mice: 80 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 80 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Eram MS, Shen Y, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-781.
[2] Eram MS, Shen Y, Szewczyk M, Wu H, Senisterra G, Li F, Butler KV, Kaniskan HÜ, Speed BA, Dela Seña C, Dong A, Zeng H, Schapira M, Brown PJ, Arrowsmith CH, Barsyte-Lovejoy D, Liu J, Vedadi M, Jin J. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-781. doi: 10.1021/acschembio.5b00839. Epub 2015 Dec 8. PMID: 26598975; PMCID: PMC4798913.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4795 mL
- 17.3974 mL
- 34.7947 mL
- 5 mM
- 0.6959 mL
- 3.4795 mL
- 6.9589 mL
- 10 mM
- 0.3479 mL
- 1.7397 mL
- 3.4795 mL

技术信息

CAS号

1831110-54-3

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H25N3O

运输

蓝冰

分子量

287.40

别名

MS023

溶解度

DMSO	50.0 mg/mL (174.0 mM)
Water	insoluble

动物实验配方

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