MS049 dihydrochloride

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MS049 dihydrochloride 

MS049 dihydrochloride 是一种高效、选择性和细胞活性的 PRMT4PRMT6 双重抑制剂,IC50 分别为 34 nM 和 43 nM。MS049 dihydrochloride 降低了 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。MS049 dihydrochloride 对 HEK293 细胞无毒,并且没有影响其的生长。

MS049 dihydrochloride

MS049 dihydrochloride Chemical Structure

CAS No. : 2095432-59-8

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MS049 dihydrochloride 的其他形式现货产品:

MS049

生物活性

MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells[1].

体外研究
(In Vitro)

MS049 dihydrochloride (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM)[1].
MS049 dihydrochloride (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells[1].
MS049 dihydrochloride is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 20 hours
Result: Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50=0.97±0.05 μM).

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50=1.4±0.1 μM) in HEK293 cells.

分子量

321.29

Formula

C15H26Cl2N2O

CAS 号

2095432-59-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Shen Y 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.

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