ESI-08

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ESI-08 

ESI-08 是一种有效的选择性 EPAC 拮抗剂，可以完全抑制 EPAC1 和 EPAC2 (IC50 为 8.4 μM) 的活性。ESI-08 选择性阻断 cAMP 诱导的 EPAC 激活，但不抑制 cAMP 介导的 PKA 激活。

ESI-08

ESI-08 Chemical Structure

CAS No. : 301177-43-5

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生物活性

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[1].

IC50 & Target

IC50: 8.4 μM (EPAC2)[1]
EPAC1[1]
体外研究
(In Vitro)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

353.48

Formula

C20H23N3OS
CAS 号

301177-43-5
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]. Chen H, et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4038-43.

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