Merck, SML1907-5MG, ESI-05

Application
ESI-05 has been used to study the effect of protein exchange directly activated by cAMP 2 on traumatic brain injury.
Biochem/physiol Actions
ESI-05 is a selective inhibitor against cAMP-regulated guanine nucleotide exhange factor (GEF) EPAC2 (Exchange factor directly activated by cAMP 2) activation by targeting an EPAC2-specific allosteric site at the interface of the two cAMP-binding domains.
ESI-05 is a selective inhibitor against cAMP-regulated guanine nucleotide exhange factor (GEF) EPAC2 (Exchange factor directly activated by cAMP 2) activation by targeting an EPAC2-specific allosteric site at the interface of the two cAMP-binding domains. ESI-05 inhibits EAPC2, but not EPAC1 or PKA, activation by cAMP in a highly potent (IC₅₀ = 430 nM; 25 μM cAMP) and cAMP-competitive manner in cell-free assays, and suppresses cAMP analog 007-AM-induced cellular Rap1 activation in EPAC2-, but not EPAC1-, expressing HEK293 transfectants.