Src kinase which associates with various intracellular membranes, where it catalyzes the transfer of phosphate from ATP to a tyrosine residue within proteins is an non-receptor class of tyrosine kinases including Src, Fyn, Yes, Fgr, Hck, Lyn, Lck and Blk. Src plays an important role in both receptor-tyrosine-kinase-mediated proliferation and transformation of the cell to a tumor phenotype. Src is phosphorylated and activated by the growth factors binding to growth factor receptors including VEGFR, PDGFR, c-met receptors, ErbB family receptors and interleukin 6 (IL-6) receptors. Activated Src transduces a signal via phosphorylation of the adaptor protein Shc to the cascade that involves Ras and the mitogen-activated protein kinase (MAPK) family member, extracellular regulated kinase (Erk). This induces transcription of the early gene c-myc and increases DNA synthesis. Src can activate signal transducer and activator of transcription 3 (STAT3) via Src and Erk kinase and induce cell transformation.
|Cat.No.||Product Name||Information||Publication||Customer Review|
|S1006||Saracatinib (AZD0530)||Saracatinib (AZD0530) is a Src inhibitor for c-Src and v-Abl with IC50 of 2.7 nM and 30 nM, respectively.||(9)||(1)|
|S2700||KX2-391||KX2-391 (KX01) is a highly selective non ATP-competitive Src inhibitor with GI50 of 9-60 nM in cancer cell lines .|
|S2202||NVP-BHG712||NVP-BHG712 is a specific inhibitor of c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM and also inhibits EphB4 and VEGFR2 with ED50 of 25 nM and 4.2 μM, respectively.|