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LFM-A13, 10 mg  

LFM-A13, 10 mg

2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide

Synonyms: LFM A13, LFMA13
potent and selective inhibitor of BTK

More details

PKI-LFMA13-010

Availability: within 3 days

260,00 €

Background: LFM-A13  is a potent inhibitor of Bruton\'s tyrosine kinase (BTK) and Janus kinase 2 (JAK2). It 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. LFM-A13 acts as an anti-leukemic agent, enhancing the chemosensitivity of BTK-positive B-lineage cells to vincristine and vinblastine.

Chemical formula C11H8Br2N2O2
Molecular weight: 360 g/mol
Purity: >97%
Appearance: Off-white solid
Solubility: soluble in ethanol
CAS number: 62004-35-7

Product specific literature references:

Mahajan S, Ghosh S, Sudbeck EA, Zheng Y, Downs S, Hupke M, Uckun FM (1999) "Rational design and synthesis of a novel anti-leukemic agent targeting Bruton\'s tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2, 5-dibromophenyl)propenamide]" J. Biol. Chem. 274(14):9587-99

Vassilev A, Ozer Z, Navara C, Mahajan S, Uckun FM (1999) "Bruton\'s tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex" J. Biol. Chem. 274(3):1646-56

Crosby D, Poole AW (2002) "Interaction of Bruton\'s tyrosine kinase and protein kinase Ctheta in platelets. Cross-talk between tyrosine and serine/threonine kinases" J. Biol. Chem. 277(12):9958-65

van den Akker, van Dijk, von Lindern et al. (2004) "The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity" Biol. Chem. 385 (5), 409-413

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.