ESI-09

Catalog No.S7499

ESI-09 Chemical Structure

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.

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  • Brain Behav Immun, 2016, 58:118-129.. ESI-09 purchased from Selleck.

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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.
Targets
EPAC2 [1] EPAC1 [1]
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

Animal Research:[2]
+ Expand
  • Animal Models: Epac1+/+ mice
  • Formulation: Dissolved in buffer saline containing 10% ethanol and 10% Tween-80
  • 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 slightly soluble or insoluble
In vivo Add solvents individually and in order:

* 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
Formula

C16H15ClN4O2

CAS No. 263707-16-0
Storage powder
in solvent
Synonyms N/A

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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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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cAMP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID