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Re: BIM and PKC inhibition



Jonas,
BIM has been reported to inhibit PKC subtypes alpha, beta1, beta2, and
gamma, with an IC50 of 0.016-0.020 uM, with no effect (up to 50 uM) on
insulin receptor-, EGF receptor-, and PDGF receptor-stimulated tyrosine
kinase activity.  (Toullec et al., The bisindolylmaleimide GF 109203X is
a potent and selective inhibitor of protein kinase C.   1991.  J. Biol.
Chem. 266, 15771.)

But, my dogma is, "the selectivity of an inhibitor is inversely
correlated with the length of time it has been on the market".  It also
inhibits protein kinase A (Ki = 2 uM).  Does anyone else know if BIM
inhibits other PKC isoforms, or other kinases?

Good luck,
Christopher

cicnasj@takas.lt wrote:

> Hallo everyone,
>
> Does anyone know, what class of PKC (conventional, novel or athipical)
> does BIM inhibit?
>
> Thanks in advance,
>
> Jonas Cicenas

-
     ___________________________________________________________
     Christopher Michael Tan
     Departments of Pharmacology & Toxicology and Medicine
     The University of Western Ontario

     Room 6L21  London Health Sciences Centre, University Campus
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