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HTScan® c-Kit Kinase Assay Kit #7755

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    Product Information

    Product Description

    The kit provides a means of performing kinase activity assays with recombinant human c-Kit kinase. It includes active c-Kit 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-KDR (Tyr996): 2,164 Daltons, GST-c-Kit Kinase: 75 KDa.

    Background

    c-Kit is a member of the subfamily of receptor tyrosine kinases that includes PDGF, CSF-1, and FLT3/flk-2 receptors (1,2). It plays a critical role in activation and growth in a number of cell types, including hematopoietic stem cells, mast cells, melanocytes, and germ cells (3). Upon binding with its stem cell factor (SCF) ligand, c-Kit undergoes dimerization/oligomerization and autophosphorylation. Activation of c-Kit results in the recruitment and tyrosine phosphorylation of downstream SH2-containing signaling components, including PLCγ, the p85 subunit of PI3 kinase, SHP2, and CrkL (4). Molecular lesions that impair the kinase activity of c-Kit are associated with a variety of developmental disorders (5), and mutations that constitutively activate c-Kit can lead to pathogenesis of mastocytosis and gastrointestinal stromal tumors (6). Tyr719 is located in the kinase insert region of the catalytic domain. c-Kit phosphorylated at Tyr719 binds to the p85 subunit of PI3 kinase in vitro and in vivo (7).

    Alternate Names

    c-Kit; high throughput; HTS; htscankit; kinase assay; KIT; screening; tyrosine kinase

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