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MS023(hydrochloride)
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(hydrochloride)图片
CAS NO:2108631-19-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt396.8
Cas No.2108631-19-0
FormulaC17H25N3O·3HCl
Solubility≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical NameN1-methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-1,2-ethanediamine, trihydrochloride
Canonical SMILESCC(C)OC1=CC=C(C2=CNC=C2CN(C)CCN)C=C1.Cl.Cl.Cl
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectively

MS023 is a type I PRMT inhibitor.

Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. Overexpression of PRMTs is implicated in various human diseases, such as cancer. Thus, selective inhibitors of PRMTs have been pursued by both academia as chemical tools for evaluating biological and therapeutic hypotheses.

In vitro: MS023 was identified to have high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but was inactive against type II and type III PRMTs, protein lysine methyltransferases as well as DNA methyltransferases. The crystal structure of PRMT6 with MS023 indicated that MS023 bound to the substrate binding site. Moreover, MS023 could potently decrease the cellular levels of histone arginine asymmetric dimethylation. In cells, MS023 also ould reduce the levels of arginine asymmetric dimethylation and increase levels of arginine monomethylation and symmetric dimethylation. Therefore, MS023 is a useful chemical tool for testing the role of type I PRMTs in health and disease [1].

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

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

Reference:
[1] M.  S. Eram, Y. Shen, M. M. Szewczyk, et al. A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases. ACS Chemical Biology 11.8.15, (2015).