产品说明书

ESI-09

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Chemical Structure| 263707-16-0 同义名 : -
CAS号 : 263707-16-0
货号 : A248229
分子式 : C16H15ClN4O2
纯度 : 98%
分子量 : 330.769
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(136.05 mM)，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：

IP 2% DMSO+2% Tween80+40% PEG300+water 3.3 mg/mL clear

PO 0.5% CMC-Na 43 mg/mL suspension

生物活性
靶点

  • EPAC1

    EPAC1, IC50:3.2 μM

  • EPAC2

    EPAC2, IC50:1.4 μM
描述 ESI-09 is a novel noncyclic nucleotide EPAC antagonist, showcasing selective inhibitory properties with IC50 values of 3.2 μM for EPAC1 and 1.4 μM for EPAC2, underscoring its potential in targeting these exchange proteins directly activated by cAMP[1].
作用机制 ESI-09 can competitively bind to EPAC.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.12mL

3.02mL

1.51mL

30.23mL

6.05mL

3.02mL
参考文献

[1]Almahariq M, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8.

[2]Gong B, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20.