Ro-31-7549, Monohydrate

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).

Cell permeable: yes

Primary Target
rat brain PKC

Product competes with ATP.

Reversible: yes

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

Toxicity: Standard Handling (A)

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

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.

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