ESI-05 is a potent EAPC2-specific antagonist that inhibits cAMP-mediated EPAC2 GEF activity with apparent IC50 of 0.43 uM.
ESI-05 inhibits Rap1 activation mediated by EAPC2, but not EPAC1.
ESI-05 competes with 8-NBD-cAMP binding with an apparent IC50 of 0.4 uM, does not significantly alter type I and II PKA holoenzyme activation in the presence and absence of 100 uM cAMP.
ESI-05 is a valuable tools for dissecting the isoform-specific functions of EPAC proteins.
