Biochem/physiol Actions

Target IC₅₀: 158 nM against rat brain PKC; 53 nM for PKCα, 195 nM for PKCβ, 163 nM for PKCβII, 213 nM for PKCγ, and 175 nM for PKCε

Reversible: yes

Product competes with ATP.

Primary Targetrat brain PKC

Cell permeable: yes

General description

A cell permeable, reversible, selective protein kinase C (PKC) inhibitor (IC₅₀ = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC. Does not inhibit the tyrosine phosphorylation or the activation of phospholipase Cγ₁. Exhibits some degree of PKC isozyme specificity (IC₅₀ = 53 nM for PKC_α, 195 nM for PKC_βI, 163 nM for PKC_βII, 213 nM for PKC_γ, and 175 nM for PKC_ε). Inhibits carbachol-evoked noradrenaline release (IC₅₀ = 600 nM).

A cell-permeable, reversible, selective protein kinase C (PKC) inhibitor that acts at the ATP binding site of PKC (IC₅₀ = 158 nM for rat brain PKC). Does not inhibit the tyrosine phosphorylation or the activation of phospholipase C_γ1 unlike staurosporine and other serine/threonine kinase inhibitors. IC₅₀ values for individual PKC isozymes are as follows: 53 nM for PKC_α, 195 nM for PKC_βI, 163 nM for PKC_βII, 213 nM for PKC_γ, and 175 nM for PKC_ε. Inhibits carbachol-evoked noradrenaline release (IC₅₀ = 0.6 µM).

Legal Information

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

Other Notes

Zhang, C., et al. 1997. J. Immunol. 158, 4968.Turner, N.A., et al. 1996. J. Neurochem. 66, 2381.Ozawa, K., et al. 1993. J. Biol. Chem. 268, 1749.Wilkinson, S.E., et al. 1993. Biochem. J. 294, 335.

Packaging

1 mg in Plastic ampoule

Reconstitution

Following initial use, aliquot and refrigerate (4°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)