Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase |
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Authors: | T Tamaoki H Nomoto I Takahashi Y Kato M Morimoto F Tomita |
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Affiliation: | 1. Via Emilia Parmense 84, Piacenza 29122, Italy;2. Department of Economic and Social Sciences, Piacenza, Italy |
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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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