GF 109203X (Bisindolylmaleimide I)

A PKC inhibitor

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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].

参考文献:
[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.

Protocol

Cell experiment [1]:
Cell lines	human platelets, Swiss 3T3 fibroblasts
Preparation method	The solubility of this compound in DMSO﹥20.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	human platelets: 500 nM, 1min
Applications	GF 109203X inhibited diC8-stimulated P47 phosphorylation in human platelets. Half-maximal inhibition (IC50) for protein kinase C (PKC) is obtained at 190nM (1 min) in human platelets. GF 109203X inhibited collagen-triggered ATP secretion as well as α- thrombin- and collagen- induced platelet aggregation. GF109203X could inhibit EGF receptor transmodulation in Swiss 3T3 Cells. GF 109203X completely reversed the inhibitory effect of PDBu with a half-maxima effect at 0.9μm in Swiss 3T3 fibroblasts.
Animal experiment [2]:
Animal models	Wistar rats
Dosage form	10 μg in 10% DMSO in saline by intraplantar (i.pl.) injection.
Application	GF109203X abolished the mechanical allodynia induced by BK (bradykinin).
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
参考文献: [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] Souza AL, Moreira FA, et al. In vivo evidence for a role of protein kinase C in peripheral nociceptive processing. Br J Pharmacol. 2002, 135(1), 239-247.