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CAS No.: 5184-64-5

ESI-05 Catalog No. CSN25735

Synonyms: NSC 116966

ESI 05 is an inhibitor of EPAC2. It can inhibit cAMP binding to EPAC2 and cAMP mediated EPAC2 guanine nucleotide exchange factor (GEF) activity (IC50 = 0.4 μM).

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技术信息

生物活性

描述ESI 05 is a selective EPAC2 inhibitor. It inhibits cAMP binding to EPAC2 and cAMP mediated EPAC2 guanine nucleotide exchange factor (GEF) activity (IC50=0.4μM)^[1]. It has been tested the ability of ESI 05 to compete with the binding of 8-NBD-cAMP to EPAC2. ESI-05 showed an increased potency with apparent IC50 of 0.4 ± 0.1μM, representing a 100- or 67-fold increase in affinity over cAMP^[2]. ESI-05 (1, 5, 10, and 25 µM) reduces activation of the GTPase RAP1 induced by the Epac-selective cAMP analog 007-AM in HEK293 cells expressing Epac2 but has no effect in HEK293 cells expressing Epac1.
参考文献

[1] Rehmann, H. Epac-inhibitors: Facts and Artefacts. Sci Rep. 2013. 3032(3).
[2] Tsalkova,T. et al. Isoform-specific antagonists of exchange proteins directly activated by cAMP. 2012. 109(45).

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6446 mL
- 18.2230 mL
- 36.4461 mL
- 5 mM
- 0.7289 mL
- 3.6446 mL
- 7.2892 mL
- 10 mM
- 0.3645 mL
- 1.8223 mL
- 3.6446 mL

技术信息

CAS号

5184-64-5

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H18O2S

运输

蓝冰

分子量

274.38

别名

NSC 116966

溶解度

DMSO	80.0 mg/mL (291.6 mM) warming

动物实验配方

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