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ESI-09 is a specific inhibitor of EPAC with IC50 values of 1.4 and 3.2 µM for EPAC2 and EPAC1, respectively [1].

cAMP/cAMP regulated guanine nucleotide exchange factor (EPAC/cAMP-GEF) is a guanine nucleotide exchange factor for small GTPases Rap1 and Rap2 in response to intracellular cAMP [2].

ESI-09 is a specific EPAC inhibitor. 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. 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 [1]. In the presence of 20 µM cAMP, ESI-09 inhibited cAMP-mediated EPAC2 and EPAC1 GEF activity with IC50 values of 4.4 and 10.8 µM, respectively [2].

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