RP-8-BROMO-BETA-PHENYL-1,N2-ETHENOGUANOSINE 3',5'-CYCLIC MONOPHOSPHOROTHIOATE SODIUM SALT HYDRATE

Description

Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (K_is = 35 and 30 nM). It less potently inhibits protein kinase A (K_i = 11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC₅₀ = 25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (K_i = 1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.

Uses

Rp-8-Br-PET-cyclic GMPS Sodium Salt is a competitive inhibitor of cGMP-dependent protein kinase (cGKI).

Biochem/physiol Actions

Rp-8-Br-PET-cGMPS is metabolically stable, competitive inhibitor of cGMP-dependent protein kinase G. Inhibits both PKG I (Ki?=?30 nM) and PKG II and blocks cGMP-gated retinal type ion channels (IC50?=?25 micromoles).

storage

Store at -20°C