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Biological Activity
BI-D1870 is a potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10–30 nM.
Targets
| RSK4 (Cell-free assay) | RSK3 (Cell-free assay) | RSK2 (Cell-free assay) | RSK1 (Cell-free assay) | |
| 15 nM | 18 nM | 24 nM | 31 nM |
| In vitro (25°C) | DMSO | 71 mg/mL (181.39 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 25.55 mL | 127.74 mL | 255.49 mL |
| 0.5 mM | 5.11 mL | 25.55 mL | 51.1 mL |
| 1 mM | 2.55 mL | 12.77 mL | 25.55 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.11 mL |
*The above data is based on the productmolecular weight 391.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A12452 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 501437-28-1 |
| Formula | C19H23F2N5O2 |
| M. Wt | 391.41 |
| Purity | >98% |
| SMILES | CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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