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MS023
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。
MS023图片
CAS NO:1831110-54-3
包装与价格：
包装价格(元)
5mg电议
25mg电议

产品介绍
MS023 是一种有效的、选择性的、细胞活性的人类 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂，对 PRMT1、PRMT3、PRMT4、PRMT6 和 PRMT8 的 IC50 分别为 30、119、83、4 和 5 nM .
Cas No.1831110-54-3
别名N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺
化学名N1-((4-(4-isopropoxyphenyl)-1H-pyrrol-3-yl)methyl)-N1-methylethane-1,2-diamine
Canonical SMILESNCCN(C)CC1=CNC=C1C2=CC=C(OC(C)C)C=C2
分子式C17H25N3O
分子量287.4
溶解度≥ 28.7mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 30, 119, 83, 4, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.

MS023 is a type I PRMTs inhibitor.

Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. PRMT overexpression has been observed in a variety of human diseases including cancer. PRMTs has been divided into three categories: type I PRMTs for catalyzing mono- and asymmetric dimethylation of arginine residues, type II PRMTs for catalyzing mono- and symmetric dimethylation of arginine residues, and type III PRMT for catalyzing only monomethylation of arginine residues.

In vitro: Previous study showed that MS023 had excellent potency for type I PRMTs but was completely inactive to both type II and type III PRMTs, protein lysine methyltransferases as well as DNA methyltransferases. Moreover, the crystal structure of PRMT6 with MS023 indicated that MS023 bound to the substrate binding site. In addition, MS023 could potently decrease the cellular levels of histone arginine asymmetric dimethylation. Furthermore, MS023 could reduce the levels of arginine asymmetric dimethylation and could also concurrently increase the cellular levels of both arginine monomethylation and symmetric dimethylation [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, MS023 is still in the preclinical development stage.

Reference:
[1] Eram MS, et al.  A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81.