Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetPKC

Cell permeable: yes

Target IC₅₀: 7.9 nM against rat brain PKC; 2.3 nM, 6.2 nM against Ca2+-dependent PKC α-isozyme and PKCβI, respectively

General description

A cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC; IC₅₀ = 7.9 nM for rat brain). Selectively inhibits Ca²⁺-dependent PKC α-isozyme (IC₅₀ = 2.3 nM) and PKC_βI (IC₅₀ = 6.2 nM). Does not affect the kinase activity of the Ca²⁺-independent PKC δ-, ε-, and ζ-isozymes even at micromolar levels. Reported to inhibit PKC_µ at higher concentrations (IC₅₀ = 20 nM). A 500 µg/ml solution of Gö 6976 (Cat. No. 365253) in anhydrous DMSO is also available.

A cell-permeable, reversible, and ATP-competitive inhibitor of protein kinase C (PKC; IC₅₀ = 7.9 nM for rat brain). Selectively inhibits Ca²⁺-dependent PKC_α-isozyme (IC₅₀ = 2.3 nM) and PKC_βI (IC₅₀ = 6.2 nM). Does not affect the kinase activity of the Ca²⁺-independent PKC δ-, ε-, and ζ-isoenzymes even at micromolar levels. A potent antagonist of HIV-1 induction.

Legal Information

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

Other Notes

Gschwendt, M., et al. 1996. FEBS Lett. 392, 77.Wenzel-Seifert, K., et al. 1994. Biochem. Biophys. Res. Commun.200, 1536.Martiny-Baron, G.M., et al. 1993. J. Biol. Chem.268, 9194.Qatsha, K.A., et al. 1993. Proc. Natl. Acad. Sci. USA90, 4674.

Packaging

1 mg in Plastic ampoule

500 µg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Warning

Toxicity: Standard Handling (A)