I942 is a specific, small molecule partial agonist of cyclic AMP sensor EPAC1 with AC50 of 50 uM, shows no effect on EPAC2. I942 inhibits cAMP-induced activation of EPAC1 in a concentration dependent manner. I942 and cAMP compete for binding to the CNB domain with similar affinities. I942 has partial agonist properties towards EPAC1, leading to activation of EPAC1, in the absence of cAMP, and inhibition of GEF activity in the presence of cAMP. I942 shows potential to suppress pro-inflammatory cytokine signalling with a reduced risk of side effects associated with general cAMP-elevating agents that activate multiple response pathways.
