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HTS002M ChemiScreen™ CXCR2 Membrane Preparation

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HTS002M
200 assays  
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      Overview

      Replacement Information

      Key Spec Table

      SpeciesHost CellsProtein Target
      Human Chem-1CXCR2 / IL-8b
      Description
      Catalogue NumberHTS002M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiScreen™ CXCR2 Membrane Preparation
      OverviewTRANSFECTION: Full-length human CXCR2 cDNA (Accession Number: M73969)
      Background InformationCXCR2 is a 7-TM G-protein coupled receptor that binds to the chemokines GROalpha, GRObeta, GROgamma, IL-8, ENA-78, NAP-2 and GCP-2 (Olson and Ley, 2002). Neutrophils, mast cells and microvascular endothelial cells express CXCR2, and interactions of CXCR2 with its ligands promotes chemotaxis of these cell types (Heidemann et al., 2003; Nilsson et al., 1999; White et al., 1998). Studies with mice lacking CXCR2 indicate that CXCR2 promotes growth of primary tumors and secondary metastases (Keane et al., 2004), and plays an essential role in hyperoxia-induced lung injury (Sue et al., 2004). In addition, cytomegalovirus encodes a CXCR2-binding chemokine, vCXC-1, that promotes neutrophil migration to infected cells (Penfold et al., 1999). Chemicon's CXCR2 Membrane Preps are ideal tools for screening for antagonists of interactions between CXCR2 and its ligands. Radiolabeled IL-8 binds to the CXCR2 membranes with a Kd of 0.075 nM. With 0.1 nM 125I-labeled IL-8, a 5-fold window of specific binding is obtained.
      References
      Product Information
      FormatMembranes
      PresentationMembranes were adjusted to 0.5 mg protein/ml in 50 mM Tris pH 7.4, 10% glycerol and 1% BSA, rapidly frozen, and stored at -80°C. One vial typically contains 1000 units, where a unit is the amount of membrane that will yield greater than 1000 cpm specific binding of 125I-labeled IL-8 (0.1 nM input concentration).
      Quality LevelMQ100
      Applications
      ApplicationHuman CXCR2 / IL-8b GPCR membrane preparation for Radioligand binding Assays.
      Key Applications
      • Radioligand binding assay
      Application NotesRadioligand binding assay.
      Biological Information
      Concentration0.5 mg/mL
      Entrez Gene Number
      Entrez Gene SummaryThe protein encoded by this gene is a member of the G-protein-coupled receptor family. This protein is a receptor for interleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein activated second messenger system. This receptor also binds to chemokine (C-X-C motif) ligand 1 (CXCL1/MGSA), a protein with melanoma growth stimulating activity, and has been shown to be a major component required for serum-dependent melanoma cell growth. This receptor mediates neutrophil migration to sites of inflammation. The angiogenic effects of IL8 in intestinal microvascular endothelial cells are found to be mediated by this receptor. Knockout studies in mice suggested that this receptor controls the positioning of oligodendrocyte precursors in developing spinal cord by arresting their migration. This gene, IL8RA, a gene encoding another high affinity IL8 receptor, as well as IL8RBP, a pseudogene of IL8RB, form a gene cluster in a region mapped to chromosome 2q33-q36.
      Gene Symbol
      • IL8RB
      • CD182
      • CMKAR2
      • CXCR-2
      • IL8RA
      • IL8R2
      • CXCR2
      • CDw128b
      GPCR ClassA
      Host CellsChem-1
      Protein TargetCXCR2 / IL-8b
      Target Sub-FamilyChemokine
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P25025 # Receptor to interleukin-8, which is a powerful neutrophils chemotactic factor. Binding of IL-8 to the receptor causes activation of neutrophils. This response is mediated via a G-protein that activate a phosphatidylinositol-calcium second messenger system. This receptor binds to IL-8 with a high affinity and to GRO/MGSA and NAP-2 also with a high affinity.
      SIZE: 360 amino acids; 40759 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      PTM: Phosphorylated upon ligand binding; which is required for desensitization.
      SIMILARITY: SwissProt: P25025 ## Belongs to the G-protein coupled receptor 1 family.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Quality AssuranceBmax for [125I]IL-8 binding: 0.93 pmol/mg protein; Kd for [125I] IL-8 binding: ~ 0.075 nM
      Usage Statement
      • Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
      Storage and Shipping Information
      Storage ConditionsMaintain frozen at -70°C for up to 2 years. Do not freeze and thaw.
      Packaging Information
      Material Size200 assays
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      HTS002M 04053252278372

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      Categories

      Life Science Research > Drug Discovery and Development > GPCR Cell Lines & Assays > GPCR Membrane Preparations
      Life Science Research > Proteins and Enzymes > GPCR Membrane Preparations