RP-8-bromo-beta-phenyl-1,N2-ethenoguanosine 3',5'-cyclic monophosphorothioate sodium salt hydrate

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.

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

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).

Store at -20°C

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[4] RONALD JGER. Activation of PDE10 and PDE11 phosphodiesterases.[J]. The Journal of Biological Chemistry, 2012: 1210-1219. DOI: 10.1074/jbc.m111.263806