SU 6656

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

SU 6656 is a small molecule selective inhibitor of the Src kinase family and induces caspase-independant cancer cell death.

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]

storage

Store at -20°C

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.