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

产品说明

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 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.
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).

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

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