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.

• Synonyme(s) : PKG Iα Inhibitor, Cell-Permeable, DT-3, RQIKIWFQNRRMKWKKLRKKKKKH, PKG Inhibitor VIII
• Formule empirique (notation de Hill): C₁₅₂H₂₅₈N₅₂O₂₈S
• Poids moléculaire : 3294.07
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: lyophilized
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic)
• Solubilité: DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PKG1α

Product competes with ATP.

Reversible: yes

Target K_i: 25 nM against protein kinase G Iα

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Séquence

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

Forme physique

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.

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable