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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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. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 5184-64-5 |
分子式 | C16H18O2S |
分子量 | 274.378 |
别名 | NSC 116966 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
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 |