A NEW INHIBITOR OF PROTEIN KINASE C, RK-286C (4'-DEMETHYLAMINO-4'-HYDROXYSTAUROSPORINE) I. SCREENING, TAXONOMY, FERMENTATION AND BIOLOGICAL ACTIVITY

HIROYUKI OSADA; HIDETOSHI TAKAHASHI; KYOKO TSUNODA; HIROO KUSAKABE; KIYOSHI ISONO

doi:10.7164/antibiotics.43.163

A NEW INHIBITOR OF PROTEIN KINASE C, RK-286C (4'-DEMETHYLAMINO-4'-HYDROXYSTAUROSPORINE)

I. SCREENING, TAXONOMY, FERMENTATION AND BIOLOGICAL ACTIVITY

HIROYUKI OSADA, HIDETOSHI TAKAHASHI, KYOKO TSUNODA, HIROO KUSAKABE, KIYOSHI ISONO

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JOURNAL FREE ACCESS

1990 Volume 43 Issue 2 Pages 163-167

DOI https://doi.org/10.7164/antibiotics.43.163

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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 μM. 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.

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