Merck, 365250-1MG, Gö 6976

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 PKCβI (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 PKCµ at higher concentrations (IC₅₀ = 20 nM). A 500 µg/ml solution of Gö 6976 (Cat. No. 365253) in anhydrous DMSO is also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PKC
Product competes with ATP.
Reversible: 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
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)