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GF 109203X

Cat. No. M3802
GF 109203X Structure
Synonym:

GO 6850

Size Price Availability Quantity
2mg USD 125.1  USD139 In stock
5mg USD 168.3  USD187 In stock
10mg USD 277.2  USD308 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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.
Concentrations 1 μM
Incubation time 48 hours
Animal Experiment
Animal models Wistar rats
Formulation 10% DMSO in saline
Dosages 10 μg
Administration i.pl
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 412.49
Formula C25H24N4O2
CAS Number 133052-90-1
Purity >98%
Solubility DMSO 79 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GF 109203X, GO 6850 supplier, PKC, inhibitors

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