Catalog No.S7499

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.

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ESI-09 Chemical Structure

ESI-09 Chemical Structure
Molecular Weight: 330.77

Validation & Quality Control

Quality Control & MSDS

Product Information

Product Description

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.
Targets EPAC2 [1] EPAC1 [1]
IC50 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]

Protocol(Only for Reference)

Kinase Assay: [3]

EPAC activity assays In brief, Purified samples containing GTP-bound Rap1 are denatured in SDS loading buffer, resolved by 15% denaturing polyacrylamide gel electrophoresis (SDS-PAGE) and analyzed by western blotting using anti-Rap1 antibodies. Samples from total cell lysates are also analyzed as controls for total Rap1 expression.

Animal Study: [2]

Animal Models Epac1+/+ mice
Formulation Dissolved in buffer saline containing 10% ethanol and 10% Tween-80
Dosages 10 mg/kg/d
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Almahariq M , et al. Mol Pharmacol. 2013, 83(1), 122-128.

[2] Gong B, et al. Proc Natl Acad Sci U S A. 2013, 110(48), 19615-19620.

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Chemical Information

Download ESI-09 SDF
Molecular Weight (MW) 330.77


CAS No. 263707-16-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 66 mg/mL (199.53 mM)
Ethanol 20 mg/mL warming (60.46 mM)
Water <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name (E)-3-(5-tert-butylisoxazol-3-yl)-2-(2-(3-chlorophenyl)hydrazono)-3-oxopropanenitrile

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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