RSK Inhibitor II-CAS 501437-28-1-Calbiochem

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一般描述

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 ?M) 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 ?M). A useful pharmacological reagent for studying RSK-mediated cellular signaling events.
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 ?M) 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 ?M).

包装

5 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

Carriere, A., et al. 2008.Curr. Biol.18,1269
Sapkota, G.P., et al. 2007.Biochem. J.401,29.
Zaru, R., et al. 2007.Nat. Immunol.8,1227.

法律信息

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

基本信息

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