TPPB has been demonstrated to activate PKC in this cell line, this effect was seen with TPPB doses in the order of 10–1,000 × g greater than those used for bryostatin-1 in the current studies. Therefore, when comparing bryostatin-1 and TPPB, a recognized APP modulator, bryostatin-1 was found to potently activate PKC-ε translocation in SH-SY5Y cells at 10−8, 10−9, and 10−10 (at 3 h).
| Cell Experiment | |
|---|---|
| Cell lines | SH-SY5Y neuroblastoma cells |
| Preparation method | Cells were grown to confluency in 10 % serum-supplemented medium. Dilutions of bryostatin-1 or TPPB were added to serum-free culture medium at various concentrations and treatments maintained for 3 h, except in time course experiments where several time points up to 24 h were taken. Pilot studies showed no change in SH-SY5Y appearance, attachment, or cell density for at least 24 h under these conditions. |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 501.54 |
| Formula | C27H30F3N3O3 |
| CAS Number | 497259-23-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
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| Protein Kinase C (19-36)
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| [Ala113]MBP(104-118)
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| [Ala107]MBP(104-118)
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM. |
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