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 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).
Biochem/physiol Actions
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
Preparation Note
Following initial use, aliquot and refrigerate (4°C). Stock solutions are stable for up to 3 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥93% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | red to red-orange |
| solubility | DMSO: 5 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | N1C(=O)C(=C(C1=O)c4c5c([n](c4)C)cccc5)c2c3c([n](c2)CCCN)cccc3 |
| InChI | 1S/C24H22N4O2/c1-27-13-17(15-7-2-4-9-19(15)27)21-22(24(30)26-23(21)29)18-14-28(12-6-11-25)20-10-5-3-8-16(18)20/h2-5,7-10,13-14H,6,11-12,25H2,1H3,(H,26,29,30) |
| InChI key | UQHKJRCFSLMWIA-UHFFFAOYSA-N |
