CycLex c-Src Kinase Assay/Inhibitor Screening Kit

Other - 1) Screening inhibitors or activators of recombinant catalytic domain of c-Src. 2) Detecting the effects of pharmacological agents on recombinant catalytic domain of c-Src.

The Src family of non-receptor protein tyrosine kinases plays critical roles in a variety of cellular signal transduction pathways, regulating such diverse processes as cell division, motility, adhesion, angiogenesis, and survival (1-3). Constitutively activated variants of Src family kinases, including the viral oncoproteins v-Src and v-Yes, are capable of inducing malignant transformation of a variety of cell types (4). Src family kinases, most notably although not exclusively Src, are frequently overexpressed and/or aberrantly activated in a variety of epithelial and non-epithelial cancers (5). Activation is very common in colorectal and breast cancers, and somewhat less frequent in melanomas, ovarian cancer, gastric cancer, head and neck cancers, pancreatic cancer, lung cancer, brain cancers, and blood cancers (5). Further, the extent of increased Src family activity often correlates with malignant potential and patient survival (5). Activation of Src family kinases in human cancers may occur through a variety of mechanisms and is frequently a critical event in tumor progression (6). Exactly how Src family kinases contribute to individual tumors remains to be defined completely, however they appear to be important for multiple aspects of tumor progression, including proliferation, disruption of cell/cell contacts, migration, invasiveness, resistance to apoptosis, and angiogenesis (1, 5). Elevated Src tyrosine kinase activity has been found in colon cancers, particularly in those metastatic to the liver. Studies of the mechanism of Src regulation suggested that Src kinase activity is downregulated by phosphorylation of a critical C-terminal tyrosine (Tyr530 in human Src) and have implied the existence of activating mutations in this C-terminal regulatory region. Irby et al. reported the identification of a truncating mutation in Src at codon 531 in 12% of cases of advanced human colon cancer tested and demonstrated that the mutation is activating, transforming, tumorigenic, and metastasis-promoting (7). The results provided, for the first time, genetic evidence that activating Src mutations may have a role in the malignant progression of human colon cancer.

The CycLex Research Product c-Src Kinase Assay/Inhibitor Screening kit is designed to measure the activities of recombinant catalytic domain of c-Src for the rapid and sensitive evaluation of inhibitors or activators. The phosphotyrosine specific monoclonal antibody used in this assay kit has been demonstrated to recognize the phosphotyrosine residue in the recombinant ?Tyrosine kinase-substrate-1?, which is efficiently phosphorylated by c-Src in vitro.

Human: 6714 Mouse: 20779

Microplate, 10X Wash Buffer, Kinase Buffer, 20X ATP HRP conjugated Detection Antibody Substrate Reagent, Stop Solution

c-Src