LFM-A13
BTK inhibitor / LFM-A13 is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC50’s = 2.5 µM (recombinant BTK) and 17.2 µM (human BTK).1,2 It has also been shown to inhibit Polo-ilke kinase (PLK) – IC50 = 61 µM for human PLK3.3 It displayed no activity (concentrations up to 278 µM) at JAK1, JAK3, HCK, EGFRK and IRK2 or CDK1-3, CHK1, IKK, MAPK1, SAPK2a and ten tyrosine kinases3.
Biochemicals & reagents
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1) Vassilev et al. (1999), Bruton’s tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex; J. Biol. Chem., 274 1646. / 2) Mahajan et al. (1999), 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]. J. Biol. Chem. 274 9587 / 3) Uckun et al. (2007) Anti-breast cancer activity of LFM-A13, a potent inhibitor of polo-like kinase (PLK). Bioorg. Med. Chem. 15 800
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TARGET: Kinase -- PATHWAY: Cytokine -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer; Inflammation