Biological Activity
Cell permeable: no', 'Primary Target
p56lck', 'Product competes with ATP.', 'Reversible: yes', 'Target IC50: 4 nM, 5 nM, 5 nM, 100 nM, against p56lck, p59fynT, Hck , and Src, respectively; 600 nM against anti-CD3-stimulated tyrosine phosphorylation of human T cells
Background
PP2 is a potent and selective inhibitor of Src-family kinases. This small molecule inhibits Lck, Fyn, and Hck with little to no effect on ZAP-70 and JAK2. Members of the Src family are involved in the regulation of cellular excitability and synaptic plasticity. Inhibition of Src family nonreceptor protein tyrosine kinases can decrease epileptiform activity, making PP2 an important compound when studying epilepsy and antiepileptic therapies.
References
[1] Hanke, J.H. et al. (1996) J Biol Chem 271, 695-701.
[2] Sanna, P.P. et al. (2000) Proc Natl Acad Sci U S A 97, 8653-7.
