ESI-05

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Chemical Structure| 5184-64-5 同义名 : NSC 116966
CAS号 : 5184-64-5
货号 : A257124
分子式 : C16H18O2S
纯度 : 98%
分子量 : 274.378
MDL号 : MFCD00091573
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(182.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.64mL

0.73mL

0.36mL

18.22mL

3.64mL

1.82mL

36.45mL

7.29mL

3.64mL
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).