epac inhibitor

EPAC inhibitors are a class of small molecule research compounds designed to inhibit the activity of Exchange Proteins Directly Activated by cAMP (EPAC1 and EPAC2). These proteins function as guanine nucleotide exchange factors (GEFs) for the small GTPases Rap1 and Rap2, mediating cAMP-signaling pathways independent of Protein Kinase A (PKA). By binding to the cAMP-binding domain (CBD), these inhibitors prevent cAMP from inducing the conformational changes necessary for GEF activity. Prominent examples include ESI-09, a pan-EPAC inhibitor, and ESI-05, which is selective for EPAC2. While these compounds are extensively used as pharmacological probes to study the role of EPAC in cancer cell migration, insulin secretion, and viral replication (including SARS-CoV-2 and Influenza A), they remain in the preclinical research stage and have not yet transitioned to clinical development as therapeutic assets.

Other names

EPAC antagonistsExchange protein directly activated by cAMP inhibitors