General description

A cell-permeable Kaempferol (Cat. No. 420345) 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 (K_i = 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.

A cell-permeable Kaempferol (Cat. No. 420345) 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 (K_i = 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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Regulatory Review (Z)