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Am J Physiol Cell Physiol 270: C1293-C1299, 1996;
0363-6143/96 $5.00
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AJP - Cell Physiology, Vol 270, Issue 5 C1293-C1299, Copyright © 1996 by American Physiological Society

ARTICLES

Calphostin C, a widely used protein kinase C inhibitor, directly and potently blocks L-type Ca channels

H. C. Hartzell and A. Rinderknecht
Department of Anatomy and Cell Biology, Emory University School of Medicine, Atlanta, Georgia 30322, USA.

Calphostin C is a widely used inhibitor of protein kinase C; in the past 4 years at least 350 articles have been published using this drug as a selective inhibitor of protein kinase C. In this paper, we show that calphostin C also potently inhibits cardiac L-type Ca channels by a mechanism that does not involve changes in adenosine 3',5'-cyclic monophosphate levels or dephosphorylation. The inhibition requires illumination by visible light during exposure to calphostin C. The Ca current (ICa) that remains after partial inhibition of ICa has the same voltage-dependent characteristics as the control current.


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