Uses
Rp-8-pCPT-Cyclic GMPS Sodium Salt acts as a stable cell-permeable analog which competetively inhibits cGMP-dependant protein kinases affecting the nervous system.
Biological Activity
rp-8-pcpt-cyclic gmps is a gmp-dependent protein kinases (cgks) inhibitor.appreciation of cgmp as a distinct intracellular second messenger is reported to be closely followed by an intensive search for effector proteins in various organisms. a cgmp-dependent protein kinase (cgk) has been found in arthropods resulting in the eventual isolation of cgk from mammalian tissues.
in vitro
previous study found that rp-8-pcpt-cyclic gmps could selectively inhibit cgk activity in intact human platelets. the ic50 value of rp-8-pcpt-cyclic gmps for cgk ii was 114-fold lower than that for cgk iα in the presence of 1 mm cgmp. in the presence of 10 mm cgmp, the ic50 values of rp-8-pcpt-cyclic gmps for cgk iα and cgk ii increased 3- and 11-fold, respectively. in addition, millimolar concentrations of rp-8-pcpt-cyclic gmps could fully activate both enzymes, a phenomenon that was observed previously for cgk ii. because substitutions at the 8-position of the guanine ring are poorly tolerated by cgk ib, these results suggested that the rp-isomer of 8-pcpt-cgmps might be a selective activator or inhibitor, respectively, of cgk ii compared to the cgk i isoforms [1].
IC 50
18.3 and 0.16 μm for cgk iα and cgk ii, respectively.
References
[1] gamm, d. m.,francis, s.h.,angelotti, t.p., et al. the type ii isoform of cgmp-dependent protein kinase is dimeric and possesses regulatory and catalytic properties distinct from the type i isoforms. the journal of biological chemisty 270(45), 27380-27388 (1995).
