ESI-09 is a specific, noncyclic nucleotide EPAC antagonist (IC50=9 uM) with no effect towards PKA.
ESI-09 specifically blocks intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells.
ESI-09 inhibits cAMP-mediated EPAC2 GEF activity and cAMP-mediated EPAC1 GEF activity with IC50 of 1.4 and 3.2 uM, respectively.
ESI-09 inhibits pancreatic cancer cell migration and invasion.
