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ESI-09 {[allProObj[0].p_purity_real_show]}

货号:A248229

ESI-09 is selective inhibitor of EPAC1 and EPAC2 with IC50 of 3.2 μM and 1.4 μM.

ESI-09 化学结构 CAS号:263707-16-0
ESI-09 化学结构
CAS号:263707-16-0
ESI-09 3D分子结构
CAS号:263707-16-0
ESI-09 化学结构 CAS号:263707-16-0
ESI-09 3D分子结构 CAS号:263707-16-0
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ESI-09 纯度/质量文件 产品仅供科研

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ESI-09 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].
体内研究

Moreover, ESI-09 treatment in wild-type (WT) mice infected with R. australis resulted in notably milder disease manifestations and significantly improved survival rates[2].

体外研究

This antagonist demonstrates enhanced efficacy in comparison to cAMP, displacing 8-NBD-cAMP binding with an apparent IC50 of 10 μM, and effectively inhibiting cAMP-mediated GEF activity of both EPAC2 and EPAC1. Additionally, ESI-09 dose-dependently suppresses 007-AM-stimulated Akt phosphorylation at T308 and S473, indicating its role in modulating key signaling pathways[1].

Beyond its anticancer potential, ESI-09 has been shown to significantly reduce both intracellular and total bacterial counts in human umbilical vein endothelial cells (HUVECs) post-infection with R. australis at a multiplicity of infection (MOI) of 10, compared to controls. This demonstrates its utility in infectious disease models, particularly in reducing bacterial burden[2].

作用机制 ESI-09 can competitively bind to EPAC.[1]

ESI-09 动物研究

Dose Rat: 1 mg/kg[2] (i.p.)
Mice: 10 mg/kg[3] (i.p.); 50 mg/kg[3] (p.o.)
Administration i.p., p.o.

ESI-09 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.

ESI-09 实验方案

计算器
存储液制备 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

ESI-09 技术信息

CAS号263707-16-0
分子式C16H15ClN4O2
分子量 330.769
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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