product name ESI-09
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, it displays >100-fold selectivity over PKA. ESI-09 (25 µM) reduced EPAC1 and EPAC2 GEF activity to basal levels in the presence of 25 µM cAMP. In the presence of 25 µM cAMP, ESI-09 inhibited cAMP-mediated EPAC2 and EPAC1 GEF activity with IC50 values of 1.4 and 3.2 µM respectively and exhibited 100 times selectivity than PKA.
References: Mol Pharmacol. 2013 Jan;83(1):122-8; Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20.
330.77
Formula
C16H15ClN4O2
CAS No.
263707-16-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (199.5 mM)
Water: <1 mg/mL
Ethanol: 20 mg/mL (60.5 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: In the pancreatic cancer cell line AsPC-1, ESI-09 inhibited Akt phosphorylation at T308 and S473 stimulated by 007-AM in a dose dependent way. In pancreatic endocrine β cells, ESI-09 inhibited the increase of insulin secretion stimulated by 007-AM in a dose dependent way. In pancreatic cancer cell lines AsPC-1 and PANC-1, ESI-09 significantly reduced cell migration through the inhibition of EPAC1. |
|---|---|
| In Vivo | ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis. |
| Animal model | Epac1+/+ mice |
| Formulation & Dosage | Dissolved in buffer saline containing 10% ethanol and 10% Tween-80; 10 mg/kg/d; i.p. injection |
| References | Mol Pharmacol. 2013 Jan;83(1):122-8; Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20; PLoS One. 2013 Dec 11;8(12):e82354. |
