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Biol Chem. 2004 May;385(5):409-13.

The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity.

Author information

1
Department of Hematology, Erasmus MC, PO Box 1738, NL-3000 DR Rotterdam, The Netherlands.

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.

PMID:
15196000
DOI:
10.1515/BC.2004.045
[Indexed for MEDLINE]

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