Chelerythrine is a potent and specific inhibitor of protein kinase C.

  title={Chelerythrine is a potent and specific inhibitor of protein kinase C.},
  author={J. J. Herbert and J. M. Augereau and J. Gleye and Jean Pierre Maffrand},
  journal={Biochemical and biophysical research communications},
  volume={172 3},
The benzophenanthridine alkaloid chelerythrine is a potent, selective antagonist of the Ca++/phospholopid-dependent protein kinase (Protein kinase C: PKC) from the rat brain. Half-maximal inhibition of the kinase occurs at 0.66 microM. Chelerythrine interacted with the catalytic domain of PKC, was a competitive inhibitor with respect to the phosphate acceptor (histone IIIS) (Ki = 0.7 microM) and a non-competitive inhibitor with respect to ATP. This effect was further evidenced by the fact that… CONTINUE READING
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