CGP 77675 (hydrate)

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.šuša, 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)