Epac activator, 5 µmol (~2,5 mg)

8-CPT-2\'-O-Me-cAMP is a selective activator of Epac (Exchange Protein directly Activated by cAMP), the cAMP-sensitive guanine nucleotide-exchange factor (cAMP-GEF) for Rap1 and Rap2. It activates Epac1 with an EC50 of 2.2 µM, but not PKA (EC50 > 10 µM). This compound stimulates Epac-mediated Ca2+-mediated Ca2+ release in pancreatic b-cells in vitro. High lipophilicity and membrane permeability as well as increased PDE stability. 

Synonyms: Epac activator, 8-CPT-2\'-O-Me-cAMP sodium salt

8-CPT-2’-O-Me-cAMP:                  order-no. PKE- EPAC-005
Chemical name.:                          8-(4-Chlorophenylthio)-2'-O-methyladenosine-3',5'-cyclic monophosphate sodium salt
CAS No.                                      634207-53-7
Formula:                                      C17H16ClN5O6PS . Na
Molecular Weight:                       507.8 g/mol
Appearance:                              white solid
Solubility:                                    water (333 mM), DMSO (333 mM), please rinse tube walls carefully and preferably use ultrasonic or vortex to achieve total and uniform mixing.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers. 

Product specific literature references:

de Rooij J, Zwartkruis FJ, Verheijen MH, Cool RH, Nijman SM, Wittinghofer A, Bos JL (1998) "Epac is a Rap1 guanine-nucleotide-exchange factor directly activated by cyclic AMP" Nature 396(6710):416-7

Kawasaki H, Springett GM, Mochizuki N, Toki S, Nakaya M, Matsuda M, Housman DE, Graybiel AM (1998) "A family of cAMP-binding proteins that directly activate Rap1" Science 282(5397):2275-9

Enserink JM, Christensen AE, de Rooij J, van Triest M, Schwede F, Genieser HG, Doskeland SO, Blank JL, Bos JL (2002) "A novel Epac-specific cAMP analogue demonstrates independent regulation of Rap1 and ERK" Nat. Cell Biol. 4(11):901-6

Christensen AE, Selheim F, de Rooij J, Dremier S, Schwede F, Dao KK, Martinez A, Maenhaut C, Bos JL, Genieser HG, Doskeland SO (2003) "cAMP analog mapping of Epac1 and cAMP kinase. Discriminating analogs demonstrate that Epac and cAMP kinase act synergistically to promote PC-12 cell neurite extension" J. Biol. Chem. 278(37):35394-402

Rangarajan S, Enserink JM, Kuiperij HB, de Rooij J, Price LS, Schwede F, Bos JL (2003) "Cyclic AMP induces integrin-mediated cell adhesion through Epac and Rap1 upon stimulation of the beta 2-adrenergic receptor" J. Cell Biol. 160(4):487-93

Rehmann H, Schwede F, Doskeland SO, Wittinghofer A, Bos JL (2003) "Ligand-mediated activation of the cAMP-responsive guanine nucleotide exchange factor Epac" J. Biol. Chem. 278(40):38548-56

Kang G, Joseph JW, Chepurny OG, Monaco M, Wheeler MB, Bos JL, Schwede F, Genieser HG, Holz GG (2003) "Epac-selective cAMP analog 8-pCPT-2\'-O-Me-cAMP as a stimulus for Ca2+-induced Ca2+ release and exocytosis in pancreatic beta-cells" J. Biol. Chem. 278(10):8279-85

Lin SL, Johnson-Farley NN, Lubinsky DR, Cowen DS (2003) "Coupling of neuronal 5-HT7 receptors to activation of extracellular-regulated kinase through a protein kinase A-independent pathway that can utilize Epac" J. Neurochem. 87(5):1076-85

Product Citations:

Bernascone S1, Erriquez J, Ferraro M, Genazzani AA, Distasi C. (2010) "Novel adenosine and cAMP signalling pathways in migrating glial cells."Cell Calcium. 48(1):83-90.