性能参数

产品名称

MS049 (hydrochloride)

规格

5mg  10mg 25mg

货号

GOY-Y3997

 含量

>98.00%

CAS

2095432-59-8

别名

化学名

N-methyl-4-(phenylmethoxy)-1-piperidineethanamine, dihydrochloride

分子式

C15H24N2O ? 2HCl

分子量

分子量 321.3

溶解度

≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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.

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