Drug intelligence / Profile preview

8-pMeOPT-2'-O-Me-cAMP

Development stage
Preclinical
Lead developer
BIOLOG Life Science Institute
Modality
Small Molecules
01

Overview

8-pMeOPT-2'-O-Me-cAMP (also known as 8-pMeOPT) is a cell-permeable, stable, and highly selective agonist of the Exchange Protein directly Activated by cAMP (Epac). It is a synthetic analog of cyclic AMP (cAMP) designed with a 2'-O-methyl modification that renders it nearly inactive toward Protein Kinase A (PKA), and an 8-para-methoxyphenylthio (pMeOPT) substitution that increases its affinity for Epac1 and Epac2. As a specialized research tool, it allows for the isolated study of Epac-mediated signaling pathways, such as those involving Rap1 activation, calcium mobilization, and cytoskeletal dynamics. In the context of oncology research, specifically melanoma, 8-pMeOPT has been used to demonstrate that Epac activation promotes cell migration through the PLCε/IP3 receptor 1 pathway and subsequent Ca2+-dependent actin assembly.

Other names
8-(4-Methoxyphenylthio)-2'-O-methyladenosine-3',5'-cyclic monophosphate8-(4-Methoxyphenylthio)-2'-O-methyl-cAMP8-pMeOPT-2'-OMe-cAMP
02

Targets

EPAC2 (Exchange factor directly activated by cAMP 2)EPAC1 (Rap guanine nucleotide exchange factor 3)

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