| 产品描述: | MS049 dihydrochloride 是一种高效、选择性和细胞活性的 PRMT4 和 PRMT6 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。 |
| 体外研究: |
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). 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. 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. |
| 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. |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.112 ml |
15.562 ml |
31.125 ml |
| 5 mM |
0.622 ml |
3.112 ml |
6.225 ml |
| 10 mM |
0.311 ml |
1.556 ml |
3.112 ml |
| 50 mM |
0.062 ml |
0.311 ml |
0.622 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |