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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 | |
| Formulation | |
| Dosages | |
| Administration | |
| 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.
| Molecular Weight | 391.42 |
| Formula | C19H23F2N5O2 |
| CAS Number | 501437-28-1 |
| Purity | >98% |
| Solubility | DMSO 68 mg/mL |
| Storage | at -20°C |
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| SL 0101-1
SL-0101-1 is a selective p90 RSK inhibitor for RSK2 with IC50 of 89 nM. |
| FMK
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants. |
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PF-4708671 is a novel cell-permeable inhibitor of S6K1 with Ki/IC50 value of 20 nM/160 nM. |
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