ESI-05 is an inhibitor of exchange protein activated by cAMP 2 (Epac2) that inhibits cAMP-induced Epac2 guanine nucleotide exchange factor (GEF) activity with an IC50 value of 0.43 ?M in a cell-free assay.1 It is selective for Epac2 over Epac1 and PKA at 25 ?M. ESI-05 (1, 5, 10, and 25 ?M) reduces activation of the GTPase RAP1 induced by the Epac-selective cAMP analog 007-AM in HEK293 cells expressing Epac2 but has no effect in HEK293 cells expressing Epac1.
1.Tsalkova, T., Mei, F.C., Li, S., et al.Isoform-specific antagonists of exchange proteins directly activated by cAMPProc. Natl. Acad. Sci. USA109(45)18613-18618(2012)