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Enzastaurin inhibits PKCβ, PKCα, PKCγ and PKCε with IC50's of 0.006, 0.039, 0.083 and 0.110 µM, respectively. Enzastaurin apparently inhibits tumor growth via multiple mechanisms: suppression of tumor cell proliferation, induction of tumor cell apoptosis and inhibition of tumor-induced angiogenesis.
| Cell Experiment | |
|---|---|
| Cell lines | PC-3 prostate cancer, HCT116 colon cancer, and U87MG glioblastoma cell lines |
| Preparation method | Proliferation assays. Proliferation was assessed for all cell lines over a 6-day time course in media supplemented with 1% FBS (7 days total). Briefly, 1,000 cells were plated per well in a 96-well plate and changed to fresh media (1% FBS) with or without enzastaurin on days 1 and 4. On day 7, the media were removed and 100 μL propidium iodide (PI) solution (10 μg/mL in D-PBS) were added to each well. An initial reading for PI staining (excitation at 500 nmol/L, absorbance at 615 nmol/L) was done using the WallacVictor plate reader following a 30-minute incubation to determine the nonviable cell fraction. The plate was then frozen at −80 °C for 2 hours, thawed, and reread. The proliferative index was scored by subtracting the prefreeze data (nonviable cells) from the postfreeze data (all cells). |
| Concentrations | 0~10µM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | Athymic nude mice bearing HCT116 colon cancer xenografts |
| Formulation | 10% acacia (Fisher Scientific, Fair Lawn, NJ) in water |
| Dosages | twice daily at 75 mg/kg |
| Administration | gavage |
| Molecular Weight | 515.61 |
| Formula | C32H29N5O2 |
| CAS Number | 170364-57-5 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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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