產(chǎn)品目錄

規(guī)格	5mg 10mg 25mg
CAS	2095432-59-8
別名
化學(xué)名	N-methyl-4-(phenylmethoxy)-1-piperidineethanamine, dihydrochloride
分子式	C15H24N2O 2HCl
分子量	321.3
溶解度	≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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