ESI-05

ESI-05 is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM) . ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation. (In Vitro) :ESI-05 (0.01 μM -1 nM) inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 0.43 μM, but completely ineffective in suppressing EPAC1 GEF activity.ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells. (In Vivo) :ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo.