For research use only.

Catalog No.S7499

7 publications

ESI-09 Chemical Structure

CAS No. 263707-16-0

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.

Selleck's ESI-09 has been cited by 7 publications

4 Customer Reviews

  • 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.

    Inhibition of Epac1 abrogated the up-regulated phosphorylation of Akt in curcumin-pretreated BMSCs during H/R injury. BMSCs were pretreated with 10 μM ESI-09 for 30 min followed by 2 h of 10 μM curcumin (CUR10) treatment, and then exposed to H/R (20/1 h) injury. (A–C) Immunoblotting analysis on the protein level changes of p-Akt and Akt (A), p-Erk1/2 and Erk1/2 (B), as well as p-p38 and p38 (C) in BMSCs following the indicated treatments. Bar graphs on the down column showing the differences after each data point of the phosphorylated form was normalized against its corresponding total protein level with the value in control was adjusted to 100%. β-actin served as loading control. Error bars represented mean ± SEM (n = 3–4). #P <  0.05, ##P <  0.01 versus control; *P <  0.05, **P <  0.01 versus H/R group; $P <  0.05 versus curcumin + H/R treatment group.

    Biomed Pharmacother, 2019, 109:1268-1275. ESI-09 purchased from Selleck.

  • Permeability of endothelial monolayers stimulated with the EPAC-1 inhibitor ESI-09 (10 µM) is increased under normoxic conditions. e miR-7 mimics increase endothelial monolayer permeability under normoxic conditions without affecting

    Acta Diabetol, 2017, 54(6):581-591. ESI-09 purchased from Selleck.

    The effect of Epac inhibitor ESI-09 (1 and 10 μM) in LPS-stimulated MLE-12.

    Inflammation, 2018, 41(3):1093-1103. ESI-09 purchased from Selleck.

Purity & Quality Control

Choose Selective cAMP Inhibitors

Biological Activity

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.
EPAC2 [1]
(Cell-free assay)
EPAC1 [1]
(Cell-free assay)
1.4 μM 3.2 μM
In vitro

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. [1] ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. [2] 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. [3]

In vivo ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis. [2]


Animal Research:[2]
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  • Animal Models: Epac1+/+ mice
  • Dosages: 10 mg/kg/d
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (199.53 mM)
Ethanol 20 mg/mL warmed (60.46 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10% ethanol+10% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 330.77


CAS No. 263707-16-0
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(C)C1=CC(=NO1)C(=O)C(=NNC2=CC(=CC=C2)Cl)C#N

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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cAMP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID