Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase

Biochem Biophys Res Commun. 1986 Mar 13;135(2):397-402. doi: 10.1016/0006-291x(86)90008-2.


Staurosporine, microbial alkaloid which has been known to have antifungal activity was found to inhibit markedly phospholipid/Ca++dependent protein kinase (protein kinase C) from rat brain, with an IC50 value of 2.7 nM. However, it had little effect on the binding of 3H-phorbol-12, 13-dibutyrate (PDBu) to protein kinase C. The inhibition of protein kinase C was not competitive with phospholipid. This compound also showed the strong cytotoxic effect on the growth of HeLa S3 cells, with an IC50 value of 4 X 10(-12)M under the condition of 72 hr-exposure.

MeSH terms

  • Alkaloids / pharmacology*
  • Animals
  • Binding, Competitive
  • Brain / enzymology
  • Cell Division / drug effects
  • HeLa Cells
  • Humans
  • Phorbol 12,13-Dibutyrate
  • Phorbol Esters / metabolism
  • Protein Binding / drug effects
  • Protein Kinase C / antagonists & inhibitors*
  • Rats
  • Staurosporine


  • Alkaloids
  • Phorbol Esters
  • Phorbol 12,13-Dibutyrate
  • Protein Kinase C
  • Staurosporine