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).
Cell Experiment | |
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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 | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 391.42 |
Formula | C19H23F2N5O2 |
CAS Number | 501437-28-1 |
Solubility (25°C) | DMSO 68 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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