ESI-09|cas 263707-16-0|DC Chemicals

ESI-09|cas 263707-16-0|DC Chemicals

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.

Product Name: ESI-09 |Catalog Number:  DC8443 | cas: 263707-16-0 | Other names: ESI-09,ESI 09,ESI09 | Chemical name：(E)-3-(5-tert-butylisoxazol-3-yl)-2-(2-(3-chlorophenyl)hydrazono)-3-oxopropanenitrile
 | Molecule Formula: C16H15ClN4O2 | MW: 330.77

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

For research and scientific purpose only, not for human use.