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Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board Member: Buchner, Johannes / Lei, Ming / Ludwig, Stephan / Sies, Helmut / Turk, Boris / Wittinghofer, Alfred

SCImago Journal Rank (SJR) 2015: 1.607
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The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity

E. van den Akker / T.B. van Dijk / U. Schmidt / L. Felida / H. Beug / B. Löwenberg / M. von Lindern

Citation Information: Biological Chemistry. Volume 385, Issue 5, Pages 409–413, ISSN (Print) 1431-6730, DOI: 10.1515/BC.2004.045, June 2005

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LFMA13, or α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, was shown to inhibit Brutons tyrosine kinase (Btk). Here we show that LFM-A13 efficiently inhibits erythropoietin (Epo)-induced phosphorylation of the erythropoietin receptor, Janus kinase 2 (Jak2) and downstream signalling molecules. However, the tyrosine kinase activity of immunoprecipitated or in vitro translated Btk and Jak2 was equally inhibited by LFM-A13 in in vitro kinase assays. Finally, Epo-induced signal transduction was also inhibited in cells lacking Btk. Taken together, we conclude that LFM-A13 is a potent inhibitor of Jak2 and cannot be used as a specific tyrosine kinase inhibitor to study the role of Btk in Jak2-dependent cytokine signalling.

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