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 (Item No. 13122) to maintain mouse embryonic stem cells.⁵

WARNING This product is not for human or veterinary use.

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 vivo. Bone 24(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 cells. Mol. Biol. Cell 13(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 inhibitor. Protein 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 survival. Transplantation 80(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 signaling. Stem Cells 30(7), 1394-1404 (2012).