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BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro. BI-D1870 does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Additionally, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB (cAMP-response-element-binding protein).
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Source | Cell Death Dis (2013). Figure 5. BI-D1870 |
| Method | FACS analyses | |
| Cell Lines | HCT116 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | BI-D1870 by itself induced massive apoptosis in p21-deficient cells, whereas wild-type and p53-/- cells were killed by this compound to a much lesser extent, suggesting a close functional relationship between RSKs and p21. |
| Cell Experiment | |
|---|---|
| Cell lines | HEK-293 cells |
| Preparation method | Prior to stimulation, cells were cultured in the absence of serum for 16 h. Inhibitors were dissolved in DMSO at a 1000-fold higher concentration than they were used at. These inhibitors, or the equivalent volume of DMSO as a control, were added to the tissue culture medium 30 min prior to stimulation, unless indi-cated otherwise. The final concentration of DMSO in the culture medium was 0.1% and had no effect on agonist-induced activ-ation or phosphorylation of any of the substrates examined. The cells were stimulated with the indicated agonists and lysed in 1 ml of ice-cold Lysis Buffer, and centrifuged at 16000 g at 4 °C for 5 min. The supernatants were frozen in liquid nitrogen and stored at −80 °C until use. Protein concentrations were determined using the Bradford method with BSA as the standard. |
| Concentrations | 10 μM |
| Incubation time | 4 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c nude mice |
| Formulation | Not Mentioned |
| Dosages | 50 mg/kg |
| Administration | Intravenous injection |
| Molecular Weight | 391.42 |
| Formula | C19H23F2N5O2 |
| CAS Number | 501437-28-1 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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