Chemical Name
9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3,2,1-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-11-(methylamino)-, [9S-(9alpha,10beta,11beta,13alpha)]-
In vitro
Staurosporine (AM-2282, SSP) can potently inhibit protein kinase C with IC50 of 2.7 nM. Staurosporine (AM-2282) can also inhibit NADPH-Oxidase activation. Besides inhibiting protein kinase C, staurosporine (AM-2282) also inhibit cyclic AMP-dependent kinase and the tyrosine kinase pp60src. In intact human neutrophils, staurosporine can potently block the action of the phorbol ester tumor promoters with nM concentrations, but shows no inhibition to the effects of phorbol 12,13-dibutyrate on epidermal growth factor binding in mouse primary epidermal cells. aurosporine is an effective inhibitor of the EGF-stimulated receptor tyrosine kinase. In both human epidermal carcinoma A431 cells and mouse Swiss 3T3 fibroblasts, staurosporine treatment causes enhancement in high affinity EGF binding and a decrease in the phosphorylation state of the unstimulated receptor.[2] Staurosporine (AM-2282, SSP) can stop progression of normal nontransformed cells in the G1 phase of the cell cycle.The target(s) of SSP is (are) either the p33cdk/cyclin E complex itself or other protein kinase(s), activated subsequent to the cyclin D but prior to the cyclin E restriction point, the activity of which is essential for cell transit through G1. Staurosporine at a concentration of 20 nM arrests normal diploid fibroblasts 3 h into G1, and staurosporine (2 nM) induces a new G1 arrest point at 6 h into G1.
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