General description
A cell-permeable Kaempferol glycoside that targets the the N-terminal kinase domain of p90 ribosomal S6 kinase and inhibits RSK kinase activity (IC50 = 89 nM with 10 µM ATP) in a selective, reversible, and ATP-competitive (Ki = 1 µM) manner. Shown to inhibit the proliferation of MCF-7, but not the normal breast cell line MCF-10A, and specifically block PDB-induced cellular phosphorylation of RSK substrate p140, but not that of RSK or RSK upstream kinases even at concentrations as high as 100 µM. Also available as a 10 mM solution in DMSO (Cat. No. 559292).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Smith, J.A., et al. 2007. Bioorg. Med. Chem.15, 5018.
Smith, J.A., et al. 2006. Bioorg. Med. Chem.14, 6043.
Xu, Y.M., et al. 2006. Bioorg. Med. Chem.14, 3974.
Maloney, D.J. and Hecht, S.M., 2005. Org. Lett.7, 1097.
Smith, J.A., et al. 2005. Cancer Res.65, 1027.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow |
| solubility | DMSO: 10 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | O1[C@H]([C@@H]([C@@H]([C@H]([C@@H]1C)OC(=O)C)OC(=O)C)O)Oc2[c](c3c([o]c2c4ccc(cc4)O)cc(cc3O)O)=O |
| InChI | 1S/C25H24O12/c1-10-21(34-11(2)26)24(35-12(3)27)20(32)25(33-10)37-23-19(31)18-16(30)8-15(29)9-17(18)36-22(23)13-4-6-14(28)7-5-13/h4-10,20-21,24-25,28-30,32H,1-3H3/t10-,20+,21-,24-,25-/m0/s1 |
| InChI key | SXOZSDJHGMAEGZ-IGKKHSBFSA-N |
