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. The solid form (Cat. No. 559285) is also available.

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.

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

500 µg in Glass bottle

Packaged under inert gas

Physical form

A 10 mM (500 µg/97 µl) solution of RSK Inhibitor, SL0101 (Cat. No. 559285) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Warning

Toxicity: Irritant (B)