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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
规格:98%
分子量:396.8
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
type I PRMTs inhibitor
CAS:2108631-19-0
分子式:C17H25N3O ? 3HCl
分子量:396.8
纯度:98%
存储:Store at -20°C

Background:

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).