HTS004M - ChemiSCREEN™ CXCR4 Chemokine Receptor Membrane Preparation

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    The chemokine SDF-1a and its GPCR receptor CXCR4 have a one-to-one specificity that is unique among chemokines and their receptors. SDF-1a 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-1a 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). CXCR4 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high level of GPCR surface expression. Thus, they are ideal tools for screening for antagonists of interactions between CXCR4 and SDF-1a. [125I]-SDF-1a binds to the CXCR4 membranes with a Kd of 0.9 nM. With 0.13 nM [125I]-SDF-1a and 5 mg/well of CXCR4 membrane preparation, a greater than 4-fold signal to background ratio is obtained.

    Additional Resource: HTS004M082514_Datasheet

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles.
    Applications: Radioligand Binding Assay
    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 signaling, 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.