Description
Exchange protein activated by cAMP (Epac) proteins mediate cAMP signaling independent of protein kinase A (PKA). HJC0197 is a cell-permeable inhibitor of Epac1 and Epac2 (IC
50 = 5.9 μM for Epac2). It inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM, but has no effect on cAMP-induced type I and II PKA activity at this concentration. Pretreatment of HEK293 cells expressing either Epac1 or Epac2 with 10 μM HJC0197 completely blocks Epac-mediated phosphorylation of Akt. HJC0197 has been used to study the role of Epac signaling in chondrogenesis in chicken micromass cultures.
Uses
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP[1].
References
[1] Chen H, et al. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4038-43. DOI:
10.1016/j.bmcl.2012.04.082
