LFM-A13
Chemical Name: 2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide
Purity: ≥98%
Biological Activity
LFM-A13 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). Inhibits recombinant BTK with an IC50 value of 2.5 μM and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μM.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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STIM1 tyrosine-phosphorylation is required for STIM1-Orai1 association in human platelets.
Lopez E, Jardin I, Berna-Erro A, Bermejo N, Salido GM, Sage SO, Rosado JA, Redondo PC
Cell. Signal., 2012;24(6):1315-22. -
Inhibitor of Tec kinase, LFM-A13, decreases pro-inflammatory mediators production in LPS-stimulated RAW264.7 macrophages via NF-?B pathway
F Wang, W Zhang, C Wang, X Fang, H Cheng, S Liu, XL Chen
Oncotarget, 2017;8(21):34099-34110. -
High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Interaction of Bruton's tyrosine kinase and protein kinase Cθ in platelets.
Crosby and Pool
J.Biol.Chem., 2002;277:9958 -
Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide].
Mahajan et al.
J.Biol.Chem., 1999;274:9587 -
Bruton's tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex.
Vassilev et al.
J.Biol.Chem., 1999;274:1646
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Citations for LFM-A13
The citations listed below are publications that use Tocris products. Selected citations for LFM-A13 include:
4 Citations: Showing 1 - 4
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Balancing tonic and phasic inhibition in hypothalamic CRH-releasing hormone neurons.
Authors: Colmers and Bains
J Physiol 2018;596:1919
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Erythropoietin Intensifies the Proapoptotic Activity of LFM-A13 in Cells and in a Mouse Model of Colorectal Cancer.
Authors: Tankiewicz-Kwedlo Et al.
Int J Mol Sci 2018;19
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NEK7 is an essential mediator of NLRP3 activation downstream of potassium efflux.
Authors: He Et al.
Nature 2016;530:354
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Essential role of Stat3 in PI3K-induced oncogenic transformation.
Authors: Hart Et al.
Pain 2011;108:13247
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