| 产品描述： | ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation |
| 靶点： |
IC50: 8.4 μM (EPAC2);EPAC1 |
| 体外研究： |
Exchange proteins directly activated by cAMP (EPAC) are a family of guanine nucleotide exchange factors that regulate a wide variety of intracellular processes in response to second messenger cAMP. ESI-08 at 25 μM has been found not to alter cAMP-induced type I and II PKA holoenzymes activation while H89, a selective PKA inhibitor, blocked the type I or II PKA activities completely |
| 参考文献： |
1. Chen H, Tsalkova T, Mei FC, Hu Y, Cheng X, Zhou J. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012;22(12):4038-4043. doi:10.1016/j.bmcl.2012.04.082 |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.829 ml |
14.145 ml |
28.29 ml |
| 5 mM |
0.566 ml |
2.829 ml |
5.658 ml |
| 10 mM |
0.283 ml |
1.414 ml |
2.829 ml |
| 50 mM |
0.057 ml |
0.283 ml |
0.566 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京