A new inhibitor of protein kinase C, RK-286C (4'-demethylamino-4'-hydroxystaurosporine). I. Screening, taxonomy, fermentation and biological activity.

Abstract

In the course of our screening program using a bleb-forming assay, a new inhibitor of protein kinase C (PKC) was found in the fermentation of a streptomycete. The inhibitor, RK-286C (4'-demethylamino-4'-hydroxystaurosporine), inhibited the morphological change of K562 cells, a human chronic erythroleukemia cell, induced by phorbol 12,13-dibutylate at the concentration of 3 microM. The same concentration of the compound inhibited the activity of PKC in vitro and the aggregation of rabbit platelets induced by collagen and arachidonic acid.

• Authors: H Osada, H Takahashi, K Tsunoda, H Kusakabe, K Isono
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 43 Issue 2 Pg. 163-7 (Feb 1990) ISSN: 0021-8820 [Print] England
• PMID: 2312404 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Alkaloids
• Anti-Bacterial Agents
• Platelet Aggregation Inhibitors
• 4'-demethylamino-4'-hydroxystaurosporine
• Protein Kinase C
• Staurosporine

Topics

• Alkaloids (isolation & purification, pharmacology)
• Animals
• Anti-Bacterial Agents (isolation & purification, pharmacology)
• Cell Membrane (drug effects, ultrastructure)
• Drug Screening Assays, Antitumor
• Fermentation
• Humans
• Male
• Microbial Sensitivity Tests
• Platelet Aggregation (drug effects)
• Platelet Aggregation Inhibitors (pharmacology)
• Protein Kinase C (antagonists & inhibitors)
• Rabbits
• Staurosporine (analogs & derivatives)
• Streptomyces (metabolism)