Molecular Weight(MW): 330.77
ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.
Cited by 2 Publications
1 Customer Review
PKA but not Epac blockade reversed the JWH133-mediated effects on the microglial phenotypic conversion. PKA (H89) or Epac (ESI-09) specific inhibitors were treated with JWH133. qPCR was used to investigate mRNA expression of the M1 markers CD86 (A) and CD68 (B), as well as the M2 markers Ym1 (D) and CD206 (E). Western blot analysis was conducted, and the relative CD68 (C) and CD206 (F) densities were evaluated for further determinations. The data are expressed as means ± SD. **P < 0.01, ***P < 0.001 vs. Throm; #P < 0.05, ##P < 0.01 vs. Throm + JWH; n = 3 per group.
Brain Behav Immun, 2016, 58:118-129.. ESI-09 purchased from Selleck.
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Choose Selective cAMP Inhibitors
|Description||ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.|
ESI-09, a novel non-cyclic nucleotide EPAC antagonist, that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently.  ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells.  ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves. 
|In vivo||ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis. |
|In vitro||DMSO||66 mg/mL (199.53 mM)|
|Ethanol||20 mg/mL warmed (60.46 mM)|
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