MS049(hydrochloride)

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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。

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	321.3
Formula	C₁₅H₂₄N₂O·2HCl
Solubility	≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Name	N-methyl-4-(phenylmethoxy)-1-piperidineethanamine, dihydrochloride
Canonical SMILES	CNCCN(CC1)CCC1OCC2=CC=CC=C2.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: 34 nM for PRMT4; 43 nM for PRMT6

MS049 is a dual PRMT4 and PRMT6 inhibitor.

PRMTs have been reported to have a key role in the regulation of the arginine methylation pattern and level of a plethora of different substrates, including both histones and non-histone proteins. Therefore, the dysregulation of PRMTs has been linked to various human diseases.

In vitro: Previous study evaluated selectivity of MS049 and its two close analogs against other PRMTs. It was found that none of these compounds showed inhibition against PRMT5 and PRMT7. In addition, all three compounds were more potent against PRMT4 and PRMT6 than other type I PRMTs. MS049 showed good selectivity over PRMT8 (>30-fold) and excellent selectivity over PRMT1 and PRMT3 (>300-fold). Moreover, MS049 could reduce the H3R2me2a mark in HEK293 cells in a concentration dependent manner. The effect of the 8 μM MS049 treatment matched with that of the catalytically inactive mutant. In addition, MS049 treatment was able to inhibit endogenous PRMT4 methyltransferase activity in a concentration dependent manner leading to reduced levels of cellular asymmetric arginine dimethylation of Med12 in HEK293 cells [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Shen Y1 et al. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Oct 13;59(19):9124-9139.