cGMP Dependent Kinase Inhibitor Peptide

Product Name:cGMP Dependent Kinase Inhibitor Peptide

Synonyms:PKG inhibitor peptide

CAS No:82801-73-8

Purity:95%

Molar Mass:943.1

Chemical Formula:C38H74N18O10

Storage:Store at -20 degrees Celsius

Sequence:RKRARKE

Application:

cGMP Dependent Kinase Inhibitor Peptide is a specialized synthetic peptide designed to specifically inhibit the activity of cGMP-dependent protein kinases (PKG). This peptide is a crucial tool in research focused on the role of PKG in various cellular processes, including vasodilation, platelet aggregation, and smooth muscle relaxation. By selectively blocking PKG activity, this inhibitor peptide allows researchers to dissect the signaling pathways regulated by cGMP, providing insights into cardiovascular function, neurological disorders, and other physiological processes. With its high purity and targeted action, this peptide ensures reliable and reproducible results in experimental studies.

Current Research:

The cGMP-dependent kinase inhibitor peptide, commonly referred to as PKG inhibitor peptide (CAS: 82801-73-8), is a synthetic heptapeptide with the sequence H₂N-Arg-Lys-Arg-Ala-Arg-Lys-Glu-OH. This peptide functions as an ATP-competitive inhibitor of cyclic guanosine monophosphate (cGMP)-dependent protein kinase, also known as protein kinase G (PKG), exhibiting a Ki value of 86 μM.

Mechanism of Action

By competing with ATP for binding to the catalytic domain of PKG, the inhibitor peptide effectively reduces the kinase's activity. This inhibition impedes the phosphorylation of PKG substrates, thereby modulating downstream signaling pathways regulated by cGMP. Notably, while the peptide competes with synthetic substrates, it does not inhibit the phosphorylation of intact histones by PKG.

Research Applications

The PKG inhibitor peptide is extensively utilized in biochemical and cellular studies to dissect the specific roles of PKG in various physiological processes, including vasodilation, platelet aggregation, and neuronal signaling. By selectively inhibiting PKG, researchers can elucidate its contributions to these pathways and explore potential therapeutic targets for conditions such as cardiovascular diseases and neurological disorders.

Considerations

When employing the PKG inhibitor peptide in experimental settings, it is crucial to consider its specificity and potential off-target effects. Appropriate controls should be implemented to ensure that observed outcomes are directly attributable to PKG inhibition. Additionally, the peptide's efficacy may vary depending on the cellular context and concentration used.

Conclusion

The cGMP-dependent kinase inhibitor peptide serves as a valuable tool for probing the functional roles of PKG in cellular signaling networks. Its application facilitates a deeper understanding of cGMP-mediated processes and supports the development of targeted therapeutic strategies.

Reference:

Chen, W., Oberwinkler, H., Werner, F., Gaßner, B., Nakagawa, H., Feil, R., … & Kuhn, M. (2013). Atrial Natriuretic Peptide–Mediated Inhibition of Microcirculatory Endothelial Ca2+ and Permeability Response to Histamine Involves cGMP-Dependent Protein Kinase I and TRPC6 Channels. Arteriosclerosis, thrombosis, and vascular biology, 33(9), 2121-2129.