hjc0350

Description: HJC0350 is a potent and selective antagonist/inhibitor of EPAC2 with IC50 of 0.3 uM, it exhibited no inhibition on Epac1. EPAC1 and EPAC2, two isoforms of exchange proteins directly activated by cAMP (EPAC), respond to the second messenger cAMP and regulate a wide variety of intracellular processes under physiological and pathophysiological circumstances. HJC 0350 competed with 8-NBD-cAMP in binding recombinant fusion protein EPAC2 with IC50 value of 0.3 uM and exhibited 133-fold more potent than cAMP, which competed with 8-NBD-cAMP in binding EPAC2 with IC50 value of 40 uM. In the presence of 25 uM cAMP, HJC 0350 (25 uM) inhibited EPAC2 GEF activity but had no effect on EPAC1-mediated Rap1-GDP exchange activity and cAMP-mediated PKA activation, which suggested that HJC 0350 was EPAC2-specific antagonist.

References: J Med Chem. 2013 Feb 14; 56(3):952-62.