An inhibitor of Src family kinases
CGP 77675 is an inhibitor of Src family kinases (SFKs) that blocks the phosphorylation of peptide substrates and autophosphorylation of purified c-Src (IC50s = 5-20 and 40 nM, respectively).1 It also inhibits the SFKs Lck and c-Yes with low nanomolar IC50 values.1,2,3 CGP 77675 is used to elucidate the role of SFKs in such processes as bone resorption, tight junction formation in epithelial cells, and allograft survival.2,1,4 It can also be used in combination with the GSK3 inhibitor CHIR99021 to maintain mouse embryonic stem cells.5
1.Missbach, M., Jeschke, M., Feyen, J., et al.A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivoBone24(5)437-449(1999) 2.Chen, Y.-H., Goodenough, D.A., and Jeansonne, B.Nonreceptor tyrosine kinase c-Yes interacts with occludin during tight junction formation in canine kidney epithelial cellsMol. Biol. Cell13(4)1227-1237(2002) 3.?u?a, M., Luong-Nguyen, N.-H., Crespo, J., et al.Active recombinant human tyrosine kinase c-Yes: expression in baculovirus system, purification, comparison to c-Src, and inhibition by a c-Src inhibitorProtein Expr. Purif.19(1)99-106(2000) 4.Zhang, Q., Fairchild, R.L., Reich, M.B., et al.Inhibition of Src kinases combined with CD40 ligand blockade prolongs murine cardiac allograft survivalTransplantation80(8)1112-1120(2005) 5.Shimizu, T., Ueda, J., Ho, J.C., et al.Dual inhibition of Src and GSK3 maintains mouse embryonic stem cells, whose differentiation is mechanically regulated by Src signalingStem Cells30(7)1394-1404(2012)
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