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ESI-05 is an inhibitor of exchange protein activated by cAMP 2 (Epac2) that inhibits cAMP-induced Epac2 guanine nucleotide exchange factor (GEF) activity with an IC50 value of 0.43 µM in a cell-free assay.1 It is selective for Epac2 over Epac1 and PKA at 25 µM. ESI-05 (1, 5, 10, and 25 µM) reduces activation of the GTPase RAP1 induced by the Epac-selective cAMP analog 007-AM in HEK293 cells expressing Epac2 but has no effect in HEK293 cells expressing Epac1.
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1. Isoform-