General description
The racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC50 ≤31 nM against RSK1, 2, 3, and 4; [ATP] = 100 µM) by targeting RSK N-terminal kinase domain in an ATP-competitive manner, while inhibiting 11 other kinases only at higher concentrations (IC50 ≥100 nM) and displaying little activity against 39 others. Shown to selectively inhibit RSK-dependent, but not RSK-independent, cellular protein phosphorylations in PMA-stimulated HEK-293 cells and EGF-stimulated Rat-2 cells (IC50 ~1 µM).
The racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC50 = 31, 24, 18, and 15 nM against RSK1, 2, 3, and 4, respectively; [ATP] = 100 µM) by targeting RSK N-terminal kinase domain in an ATP-competitive manner, while inhibiting 11 other kinases only at higher concentrations (IC50 ≥100 nM) and displaying little activity against 39 others. Shown to selectively inhibit RSK-dependent, but not RSK-independent, cellular protein phosphorylations in PMA-stimulated human HEK-293 cells and EGF-stimulated rat Rat-2 cells (IC50 ~1 µM). A useful pharmacological reagent for studying RSK-mediated cellular signaling events.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Carriere, A., et al. 2008. Curr. Biol.18, 1269Sapkota, G.P., et al. 2007. Biochem. J.401, 29.Zaru, R., et al. 2007. Nat. Immunol.8, 1227.
Packaging
5 mg in Glass bottle
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
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