K-252a, a potent inhibitor of protein kinase C from microbial origin

J Antibiot (Tokyo). 1986 Aug;39(8):1059-65. doi: 10.7164/antibiotics.39.1059.

Abstract

K-252a, a metabolite isolated from the culture broth of Nocardiopsis sp. K-252a, was found to exhibit an extremely potent inhibitory activity on protein kinase C. The IC50 value was 32.9 nM.

MeSH terms

  • Actinomycetales / metabolism
  • Animals
  • Bacteria / drug effects
  • Calmodulin / antagonists & inhibitors
  • Carbazoles / isolation & purification*
  • Carbazoles / pharmacology
  • Fermentation
  • Indole Alkaloids
  • Mice
  • Phosphodiesterase Inhibitors / pharmacology
  • Protein Kinase C / antagonists & inhibitors*

Substances

  • Calmodulin
  • Carbazoles
  • Indole Alkaloids
  • Phosphodiesterase Inhibitors
  • staurosporine aglycone
  • Protein Kinase C