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Usage

Uses

Used in Research Applications:
8-pCPT-2μ-O-Me-cAMP is used as a research tool for elucidating the roles of Epac1 and Epac2 in various cell functions. Its strong selectivity and activation properties make it an invaluable compound for studying the signaling pathways and cellular responses mediated by these Rap GEFs.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, 8-pCPT-2μ-O-Me-cAMP is used as a lead compound for the development of novel therapeutics targeting Epac-dependent pathways. Its ability to selectively activate Epac over PKA makes it a promising candidate for the treatment of various diseases and conditions where Epac-mediated signaling is implicated.
Used in Cell Signaling Studies:
8-pCPT-2μ-O-Me-cAMP is employed as a specific activator of Epac proteins in cell signaling studies. This allows researchers to investigate the intricate relationships between cAMP, Epac, and Rap GTPases, as well as their roles in cellular processes such as proliferation, differentiation, and apoptosis.
Used in Drug Discovery and Development:
8-pCPT-2μ-O-Me-cAMP serves as a starting point for the design and synthesis of new drugs targeting Epac-mediated pathways. Its unique properties make it a valuable template for the development of more potent and selective Epac agonists, which could potentially be used to treat a range of diseases and conditions related to cAMP signaling dysregulation.

Biological Activity

8-cpt-2me-camp, sodium salt is a selective agonist of epac [1].cyclic amp guanine nucleotide exchange factors (epacs) are intracellular sensors for camp and function as nucleotide exchange factors for the ras gtpase homologues rap1 and rap2 [1].8-cpt-2me-camp, sodium salt is a selective epac agonist. 8-cpt-2me-camp increased rap1 activation by epac1. meantime, light chain 2 (lc2) of the microtubule-associated protein map1a increased this response. in lc2- and epac1-transfected cells, 8-cpt-2me-camp increased cell adhesion to laminin [1]. in jurkat tcells, 8-cpt-2me-camp (100 μm) activated rap1, which was not affected by h-89, a pka inhibitor [2]. in 1-ln prostate cancer cells, 8-cpt-2me-camp increased epac1, p-akts473 and p-aktt308 in a dose-dependent way. 8-cpt-2me-camp increased p-akts473 and akts473 kinase activity by two-three fold. also, 8-cpt-2me-camp activated mtorc1 and mtorc2 [3].in human prostate cancer cells, 8-cpt-2me-camp increased the levels of p-cpla2s505, cox-2 and pge2. however, cox-2, ep4 or mtor inhibitors inhibited this effect and reduced protein and dna synthesis induced by epac1. these results suggested epac1 was a pro-inflammatory modulator and promoted cell proliferation [4].

Biochem/physiol Actions

Analog of natural cAMP, potent and specific membrane-permeant activator of exchange factors directly activated by cAMP (Epac or cAMP-GEF), a new receptor for cyclic AMP

references

[1]. gupta m, yarwood sj. map1a light chain 2 interacts with exchange protein activated by cyclic amp 1 (epac1) to enhance rap1 gtpase activity and cell adhesion. j biol chem, 2005, 280(9): 8109-8116. [2]. fuld s, borland g, yarwood sj. elevation of cyclic amp in jurkat t-cells provokes distinct transcriptional responses through the protein kinase a (pka) and exchange protein activated by cyclic amp (epac) pathways. exp cell res, 2005, 309(1): 161-173.[3]. misra uk, pizzo sv. upregulation of mtorc2 activation by the selective agonist of epac, 8-cpt-2me-camp, in prostate cancer cells: assembly of a multiprotein signaling complex. j cell biochem, 2012, 113(5): 1488-1500.[4]. misra uk, pizzo sv. evidence for a pro-proliferative feedback loop in prostate cancer: the role of epac1 and cox-2-dependent pathways. plos one, 2013, 8(4): e63150.