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HTScan® HER2/ErbB2 Kinase Assay Kit #7058

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    Product Information

    Product Description

    The kit provides a means of performing kinase activity assays with recombinant human HER2/ErbB2 kinase. It includes active HER2/ErbB2 kinase (supplied as a GST fusion protein), a biotinylated peptide substrate and a phospho-tyrosine antibody for detection of the phosphorylated form of the substrate peptide.
    Molecular Formula Peptide substrate, Biotin-FLT3 (Tyr589) peptide: 1,945 Daltons. GST-HER2/ErbB2 Kinase: 116 kDa.

    Background

    The ErbB2 (HER2) proto-oncogene encodes a 185 kDa transmembrane, receptor-like glycoprotein with intrinsic tyrosine kinase activity (1). While ErbB2 lacks an identified ligand, ErbB2 kinase activity can be activated in the absence of a ligand when overexpressed and through heteromeric associations with other ErbB family members (2). Amplification of the ErbB2 gene and overexpression of its product are detected in almost 40% of human breast cancers (3). Binding of the c-Cbl ubiquitin ligase to ErbB2 at Tyr1112 leads to ErbB2 poly-ubiquitination and enhances degradation of this kinase (4). ErbB2 is a key therapeutic target in the treatment of breast cancer and other carcinomas and targeting the regulation of ErbB2 degradation by the c-Cbl-regulated proteolytic pathway is one potential therapeutic strategy. Phosphorylation of the kinase domain residue Tyr877 of ErbB2 (homologous to Tyr416 of pp60c-Src) may be involved in regulating ErbB2 biological activity. The major autophosphorylation sites in ErbB2 are Tyr1248 and Tyr1221/1222; phosphorylation of these sites couples ErbB2 to the Ras-Raf-MAP kinase signal transduction pathway (1,5).

    Alternate Names

    enzyme; ErbB2; HER-2; HER2; high throughput; HTS; kinase assay; neu; Tyrosine Kinase

    For Research Use Only. Not for Use in Diagnostic Procedures.
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