RSK Inhibitor, SL0101

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.

Packaged under inert gas

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

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

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.

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

Toxicity: Irritant (B)