Staurosporine, a Potent Inhibitor of Phospholipid/Ca++dependent Protein Kinase

Overview

Journal Biochem Biophys Res Commun

Publisher Elsevier

Specialty Biochemistry

Date 1986 Mar 13

PMID 3457562

Citations 515

Authors

T Tamaoki

H Nomoto

I Takahashi

Y Kato

M Morimoto

F Tomita

Affiliations

Soon will be listed here.

Abstract

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.

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