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Overview
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Background
GF 109203X is a potent and selective inhibitor of protein kinase C [1].
Protein kinase C (PKC) is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of serine and threonine amino acid residues on target proteins. PKC enzymes are activated by increases in the concentration of Ca2+ or diacylglycerol (DAG).
GF 109203X is a competitive inhibitor with Ki value of 14 nM. It inhibited PKC with IC50 values of 0.020, 0.017, 0.016, 0.020 μM for α, βI, βII and γ, respectively. In human platelets and Swiss 3T3 fibroblasts, GF 109203X significantly inhibited PKC-mediated phosphorylations with Mr of 47000 and 80000 in platelets and Swiss 3T3 cells, respectively. Also, GF 109203X inhibited collagen-triggered ATP secretion as well as α- thrombin- and collagen- induced platelet aggregation [1]. GF 109203X selectively inhibited PKC activity extracted from either fibroblasts or keratinocytes with IC50 values of 0.01 μM and 0.4 μM, respectively. Also, GF 109203X inhibited the expression of c-fos and c-jun, which involved in the cellular differentiation process [2].[1]. Toullec D, Pianetti P, Coste H, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem, 1991, 266(24): 15771-15781.
[2]. Le Panse R, Coulomb B, Mitev V, et al. Differential modulation of human fibroblast and keratinocyte growth by the protein kinase C inhibitor GF 109203X. Mol Pharmacol, 1994, 46(3): 445-451.
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