370655

PKG Iα Inhibitor, Cell-Permeable

The PKG Iα Inhibitor, Cell-Permeable controls the biological activity of PKG Iα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PKG Iα Inhibitor, Cell-Permeable, DT-3, RQIKIWFQNRRMKWKKLRKKKKKH, PKG Inhibitor VIII
• Empirical Formula (Hill Notation): C₁₅₂H₂₅₈N₅₂O₂₈S
• Molecular Weight: 3294.07
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: lyophilized
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

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.

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PKG1α

Product competes with ATP.

Reversible: yes

Target K_i: 25 nM against protein kinase G Iα

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

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

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.

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable