Calcium Flux Assay

HTS004RTA - Ready-to-Assay™ CXCR4 Chemokine Receptor Frozen Cells

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    The chemokine SDF-1α and its GPCR receptor CXCR4 have a one-to-one specificity that is unique among chemokines and their receptors. SDF-1α binds to CXCR4 expressed on hematopoietic and lymphopoietic cells, and directs their trafficking to and retention in hemato-and lymphatopoietic organs and sites of inflammation (Kucia et al., 2004). CXCR4 is expressed on several tumor cell lineages, and might be responsible for metastasis to sites of SDF-1α expression, such as bone and lymph nodes (Muller et al., 2001). In addition, CXCR4 is a coreceptor for the HIV envelope glycoprotein gp120 (Feng et al., 1996). Small molecule antagonists of CXCR4 have been developed and shown to inhibit infectivity of T-tropic HIV strains and to impair growth of brain tumors (Arakaki et al., 1999; Rubin et al., 2003).  Cloned human CXCR4-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CXCR4 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists and modulators at CXCR4.

    Additional Resource: HTS004RTA091714_Datasheet

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    Item Unit of Measure: PK
    Contents: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Entrez Gene Number: M99293
    Protein Targets: CXCR4
    Target Sub-family: Chemokine
    Species: Human
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein
    Exogenous Gene Expression: CXCR4 cDNA (Accession Number: M99293) expressed from a proprietary pHS plasmid.
    Related Product Number: HTSCHEM-1RTA, HTS004M
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Arakaki R et al. (1999) T134, a small-molecule CXCR4 inhibitor, has no cross-drug resistance with AMD3100, a CXCR4 antagonist with a different structure. J Virol. 73: 1719-23
    Reference 2: 2. Feng Y et al. (1996) HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science 272: 872-7.
    Reference 3: 3. Kucia M et al. (2004) CXCR4-SDF-1 signalling, locomotion, chemotaxis and adhesion. J. Mol. Histol. 35: 233-45
    Reference 4: 4. Muller A et al. (2001) Involvement of chemokine receptors in breast cancer metastasis. Nature 410: 50-6.
    Reference 5: 5. Rubin JB et al. (2003) A small-molecule antagonist of CXCR4 inhibits intracranial growth of primary brain tumors. Proc. Natl. Acad. Sci. USA. 100: 13513-8.