Merck, 370655-1MG, PKG Iα Inhibitor, Cell-Permeable

General description
A highly potent, reversible, and substrate competitive membrane-permeable peptide that selectively inhibits protein kinase G Iα (PKG Iα) (Ki = 25 nM). Inhibitor peptide is fused to the Drosophila Antennapedia homeo domain peptide to allow membrane permeability. Shown to efficiently cross the membrane of arterial smooth muscle cells and inhibit nitric oxide-induced (NO-induced) vasodilation (EC₅₀ = 47 µM). Inhibits protein kinase A (PKA) activity only at much higher concentrations (Ki = 493 µM). The carrier peptide is also available under Cat. no. 287895.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PKG1α
Product competes with ATP.
Reversible: yes
Target Ki: 25 nM against protein kinase G Iα
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
Other Notes
Dostmann, W. R.G., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 14772.
H-Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Leu-Arg-Lys-Lys-Lys-Lys-Lys-His-OH
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)