MS023

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Chemical Structure| 1831110-54-3 同义名 : -
CAS号 : 1831110-54-3
货号 : A604225
分子式 : C17H25N3O
纯度 : 99%+
分子量 : 287.4
MDL号 : MFCD29924734
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.79mL

6.96mL

3.48mL
参考文献

[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.