Chemical Name:2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide
Biological Activity:
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.
Mahajanet 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. Vassilevet al (1999)
Bruton's tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing
signaling complex. J.Biol.Chem. 274 1646. Crosby and Poole
(2002) Interaction of Bruton's tyrosine kinase and protein kinase Cq in platelets. J.Biol.Chem. 277
9958.