別名

Ro-31-7549, Monohydrate - CAS 125313-65-7 - Calbiochem,2-[1-3(Aminopropyl)indol-3-yl]-3(1-methyl-1H-indol-3-yl)maleimide, Acetate, Bisindolylmaleimide VIII, Acetate

一般描述

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 PKCα, 195 nM for PKCβI, 163 nM for PKCβII, 213 nM for PKCγ, and 175 nM for PKCε). 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 Cγ1 unlike staurosporine and other serine/threonine kinase inhibitors. IC50 values for individual PKC isozymes are as follows: 53 nM for PKCα, 195 nM for PKCβI, 163 nM for PKCβII, 213 nM for PKCγ, and 175 nM for PKCε. Inhibits carbachol-evoked noradrenaline release (IC50 = 0.6 μM).

生化/生理作用

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

重懸

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

其他說明

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.