Molecular Formula | C22H21F2N3O |
Molar Mass | 381.42 |
Density | 1.257±0.06 g/cm3(Predicted) |
Boling Point | 481.1±45.0 °C(Predicted) |
Solubility | DMSO: ≥ 31 mg/mL |
pKa | 5.86±0.25(Predicted) |
Storage Condition | -20℃ |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.622 ml | 13.109 ml | 26.218 ml |
5 mM | 0.524 ml | 2.622 ml | 5.244 ml |
10 mM | 0.262 ml | 1.311 ml | 2.622 ml |
5 mM | 0.052 ml | 0.262 ml | 0.524 ml |
biological activity | LJH685 is a potent, selective, ATP-competitive RSK inhibitor, inhibition of RSK1/2/3 biological activity, IC50 6, 5, 4 nM. |
Target | IC50: 6 nM (RSK1), 5 nM (RSK1), 4 nM (RSK1) |
Cell Line: | MDA-MB-231, H358 cells MDA-MB-231, H358 cells |
Concentration: | 0.01, 0.1, 1, 10, 100 μM 0.1, 0.3, 1, 3, 10 μM |
Incubation Time: | 72 hours 4 hours |
Result: | The growth in soft agar was efficiently inhibited with EC 50 values of 0.73 and 0.79 μM in MDA-MB-231 and H358, respectively. Efficiently reduced phosphorylation of YB1 at submicromolar concentrations and caused nearly complete inhibition at higher concentrations. |