Biological Activity
Selective inhibitor of ribosomal S6 kinase (RSK) (IC50 = 89 nM for RSK2). Does not inhibit upstream kinases such as MEK, Raf and PKC. Inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
Technical Data
| M. Wt | 516.46 |
| Formula | C25H24O12 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 77307-50-7 |
| PubChem ID | 14825856 |
| InChI Key | SXOZSDJHGMAEGZ-UHFFFAOYSA-N |
| Smiles | O=C1C3=C(C=C(O)C=C3O)OC(C4=CC=C(O)C=C4)=C1OC2C(O)C(OC(C)=O)C(OC(C)=O)C(C)O2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.16 | 10 | |
| ethanol | 10.33 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 516.46. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.94 mL | 9.68 mL | 19.36 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.87 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Smith et al (2005) Identification of the first specific inhibitor of p90 ribosomal S6 kinase (RSK) reveals an unexpected role for RSK in cancer cell proliferation. Cancer Res. 65 1027 PMID: 15705904
Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214
Godeny and Sayeski (2006) ERK1/2 regulates ANG II-dependent cell proliferation via cytoplasmic activation of RSK2 and nuclear activation of elk1. Am.J.Cell.Physiol. 291 1308 PMID:
Saha et al (2012) RSK phosphorylates SOS1 creating 14-3-3-docking sites and negatively regulating MAPK activation. Biochem.J. 447 159 PMID: 22827337
Keywords: SL 0101-1, supplier, Selective, p90, ribosomal, S6, kinases, RSK, inhibitors, inhibits, SL0101-1, RSK, RSK, Tocris Bioscience
