Uses
ESI 09 acts as an EPAC inhibitor, preventing EPAC-mediated insulin release form β-pancreatic cells. Selective control for EPAC over PKA and decreases migration and invasion of AsPc-1 and PANC-1 pancreatic cancer cells.
Biochem/physiol Actions
ESI-09 is a potent, specific inhibitor of EPAC (exchange protein directly activated by cAMP). ESI-09 inhibits EPAC1 and EPAC2 with IC50 values of 3.2 and 1.4 μM, respectively, with no activity against PKA at 25 μM. In pancreatic cell lines, the compound blocks phosphorylation of Akt and insulin secretion. ESI-09 inhibits migration of pancreatic cancer cell lines.
