Description
The Src family of proto-oncogenic kinases include nine mammalian non-receptor tyrosine kinases that are involved in intracellular signaling and are often relevant to carcinogenesis. SU6656 is a selective inhibitor of Src kinases, Including Src, Yes, Lyn, and Fyn (IC50 = 280, 20, 130, 170 nM, respectively). It weakly inhibits some other kinases when used at >10 μM. SU6656 has been used to study the role of Src kinases in cell growth and development in diverse processes, including nervous system development, fibrosis, and cancer.
Uses
The Src family of proto-oncogenic kinases include nine mammalian non-receptor tyrosine kinases that are involved in intracellular signaling and are often relevant to carcinogenesis. SU6656 is a selective inhibitor of Src kinases, Including Src, Yes, Lyn, and Fyn (IC50 = 280, 20, 130, 170 nM, respectively). It weakly inhibits some other kinases when used at >10 μM. SU6656 has been used to study the role of Src kinases in cell growth and development in diverse processes, including nervous system development, fibrosis, and cancer.
General Description
A potent, cell-permeable, reversible, and ATP-competitive inhibitor of Src-family protein tyrosine kinases. Inhibits Src (IC50 = 280 nM) as well as closely related kinases Fyn (IC50 = 170 nM), Yes (IC50 = 20 nM) and Lyn (IC50 = 130 nM). The inhibition is competitive with respect to ATP. Has only a trivial effect on Lck (IC50 = 6.88 μM). Does not affect the activity of PDGF-β receptor kinase (IC50 ≥10 μM) and IGF-1 receptor kinase (IC50 ≥20 μM).
Biochem/physiol Actions
Cell permeable: yes
in vivo
su6656 administered prior to irradiation significantly promotes radiation-induced destruction of blood vessels within the tumor windows. it also facilitates tumor growth delay when administered during fractionated irradiation. [3]
References
1. blake ra, broome ma, liu x et al. su6656, a selective src family kinase inhibitor, used to probe growth factor signaling. mol cell biol. 2000 dec;20(23):9018-27.2. lannutti bj, blake n, gandhi mj et al. induction of polyploidization in leukemic cell lines and primary bone marrow by src kinase inhibitor su6656. blood. 2005 may 15;105(10):3875-8.3. cuneo kc, geng l, tan j et al. src family kinase inhibitor su6656 enhances antiangiogenic effect of irradiation. int j radiat oncol biol phys. 2006 mar 15;64(4):1197-203.
