| Literature DB >> 15196000 |
Emile van den Akker1, Thamar B van Dijk, Uwe Schmidt, Lamberto Felida, Hartmut Beug, Bob Löwenberg, Marieke von Lindern.
Abstract
LFM-A13, or alpha-cyano-beta-hydroxy-beta-methyl-N-(2,5-dibromophenyl)propenamide, was shown to inhibit Bruton's 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.Entities:
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Year: 2004 PMID: 15196000 DOI: 10.1515/BC.2004.045
Source DB: PubMed Journal: Biol Chem ISSN: 1431-6730 Impact factor: 3.915