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 (IC
50 = 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).
References
[1] E BUTT. Inhibition of cyclic GMP-dependent protein kinase-mediated effects by (Rp)-8-bromo-PET-cyclic GMPS.[J]. British Journal of Pharmacology, 1995, 116 8: 3110-3116. DOI:
10.1111/j.1476-5381.1995.tb15112.x[2] NADEJDA VALTCHEVA. The commonly used cGMP-dependent protein kinase type I (cGKI) inhibitor Rp-8-Br-PET-cGMPS can activate cGKI in vitro and in intact cells.[J]. The Journal of Biological Chemistry, 2009, 284 1: 556-562. DOI:
10.1074/jbc.m806161200[3] JI-YE WEI. Identification of Competitive Antagonists of the Rod Photoreceptor cGMP-Gated Cation Channel: β-Phenyl-1,N2-etheno-Substituted cGMP Analogues as Probes of the cGMP-Binding Site[J]. Biochemistry Biochemistry, 1996, 35 51: 16815-16823. DOI:
10.1021/bi961763v[4] RONALD JGER. Activation of PDE10 and PDE11 phosphodiesterases.[J]. The Journal of Biological Chemistry, 2012: 1210-1219. DOI:
10.1074/jbc.m111.263806
