GF 109203X is selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). GF 109203X is a potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM). GF 109203X was a competitive inhibitor with respect to ATP (Ki = 14 +/- 3 NM) and displayed high selectivity for PKC as compared to five different protein kinases. GF 109203X inhibited collagen- and alpha-thrombin-induced platelet aggregation as well as collagen-triggered ATP secretion. GF 109203X reversed the inhibition of epidermal growth factor binding induced by phorbol 12,13-dibutyrate and prevented [3H] thymidine incorporation into DNA, only when this was elicited by growth promoting agents which activate PKC. GF 109203X was thought as a new type of compound interacting with P-gp directly, but does not support the concept of a major contribution of PKC to a P-gp-associated MDR, at least using the particular cellular model systems and the selective, albeit general, PKC inhibitor GF 109203X.
|Cell lines||SNU-407 colon cancer cells|
|Preparation method||Monitoring cell proliferation by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Seeding cells in 96-well plates and allowing to grow overnight. Serum-starving the cells for 18–24 hours and then treating with 1 mM carbachol for 48 hours in 100 μL serum-free RPMI 1640. Adding inhibitors 30 min prior to carbachol treatment. Following the treatment, applying 10 μL of MTT solution (5 mg/ml) to each well, and incubating the plates for 3 h at 37 °C. After removing the medium, the formazan crystals formed are solubilized in 100 μL DMSO. Using a microplate reader to measure the absorbance at 570 nm and subtract the background absorbance at 690 nm . Each assay is performed in triplicate.|
|Incubation time||48 hours|
|Animal models||Wistar rats|
|Formulation||10% DMSO in saline|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
EGFR and PKC are involved in the activation of ERK1/2 and p90 RSK and the subsequent proliferation of SNU-407 colon cancer cells by muscarinic acetylcholine receptors.
Park YS, et al. Mol Cell Biochem. 2012 Nov;370(1-2):191-8. PMID: 22865467.
Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance.
Gekeler V, et al. Br J Cancer. 1996 Sep;74(6):897-905. PMID: 8826855.
The specific bisindolylmaleimide PKC-inhibitor GF 109203X efficiently modulates MRP-associated multiple drug resistance.
Gekeler V, et al. Biochem Biophys Res Commun. 1995 Jan 5;206(1):119-26. PMID: 7818510.
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
Toullec D, et al. J Biol Chem. 1991 Aug 25;266(24):15771-81. PMID: 1874734.
|Related PKC Products|
Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
|Zoledronic acid monohydrate
Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
Ingenol Mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
|Phorbol 12-myristate 13-acetate
Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
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