Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetPKG1α

Target K_i: 25 nM against protein kinase G Iα

Cell permeable: yes

General description

A highly potent, reversible, and substrate competitive membrane-permeable peptide that selectively inhibits protein kinase G Iα (PKG Iα) (K_i = 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 (K_i = 493 µM). The carrier peptide is also available under Cat. no. 287895.

A highly potent, reversible, and substrate competitive membrane-permeable Drosophila Antennapedia homeodomain fused-peptide that selectively inhibits protein kinase G Iα (K_i = 25 nM). Shown to efficiently translocate into arterial smooth muscle cells and inhibit NO-induced vasodilation (ED₅₀ = 47 µM). Inhibits protein kinase A at much higher concentrations (K_i = 493 µM). The carrier peptide is also available under Cat. no. 287895.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Dostmann, W. R.G., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 14772.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Sequence

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

Warning

Toxicity: Standard Handling (A)