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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 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 |
| Molecular Weight | 412.49 |
| Formula | C25H24N4O2 |
| CAS Number | 133052-90-1 |
| Solubility (25°C) | DMSO 79 mg/mL |
| Storage | 2-8°C, protect from light |
| Related PKC Products |
|---|
| Sapintoxin D
Sapintoxin D is a fluorescent phorbol ester that can be used to study the activation of protein kinase C (PKC). |
| Bryostatin 3
Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. |
| Ruboxistaurin mesylate
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. |
| PKC β pseudosubstrate
PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC. |
| Protein Kinase C (19-31)
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), is used as protein kinase C substrate peptide for testing the protein kinase C activity. |
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