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. 2011 Dec 25;8(2):141-3.
doi: 10.1038/nchembio.761.

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

Solveigh C Koeberle  1 , Johannes Romir, Stefan Fischer, Andreas Koeberle, Verena Schattel, Wolfgang Albrecht, Christian Grütter, Oliver Werz, Daniel Rauh, Thilo Stehle, Stefan A Laufer
Affiliations

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

Solveigh C Koeberle et al. Nat Chem Biol. .

Abstract

Until now, a lack of inhibitors with high potency and selectivity in vivo has hampered investigation of the p38 mitogen-activated protein kinase (MAPK) signaling pathway. We describe the design of skepinone-L, which is, to our knowledge, the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, skepinone-L is a valuable probe for chemical biology research, and it may foster the development of a unique class of kinase inhibitors.

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