Staurosporine-related compounds, K252a and UCN-01, inhibit both cPKC and nPKC.

Abstract:

:The potent inhibitors of protein kinase C (PKC), H7, staurosporine, and staurosporine derivatives, were examined for their inhibitory effects on novel PKC (nPKC) isozymes delta and epsilon. H7 and staurosporine, usually used as selective inhibitors of PKC, showed similar inhibitory effects on cPKC (a mixture of cPKC alpha, beta, and gamma) and nPKC delta and epsilon. The inhibitory effects of K252a, a non-selective protein kinase inhibitor, on cPKC was 3.2- and 22-fold higher than those on nPKC epsilon and delta, respectively. The staurosporine derivatives UCN-01 and UCN-01-Me also showed selective inhibition of cPKC.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Mizuno K,Saido TC,Ohno S,Tamaoki T,Suzuki K

doi

10.1016/0014-5793(93)80254-r

subject

Has Abstract

pub_date

1993-09-13 00:00:00

pages

114-6

issue

2

eissn

0014-5793

issn

1873-3468

pii

0014-5793(93)80254-R

journal_volume

330

pub_type

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