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HTS004M Sigma-AldrichChemiSCREEN™ CXCR4 Membrane Preparation

Human CXCR4 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.

ChemiSCREEN™ CXCR4 Membrane Preparation MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

SDS
CoA
References
Brochures
Protocols

Host Cell: Chem-1 Uni Prot Number: P61073 Entrez Gene Number: NM_001008540.1, NM_003467.2

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Overview

Replacement Information

Key Spec Table

Species	Host Cells	Protein Target
Human	Chem-1	CXCR4

Description
Catalogue Number	HTS004M
Brand Family	Chemicon®
Trade Name	ChemiScreen Chemicon
Description	ChemiSCREEN™ CXCR4 Membrane Preparation
Overview	Full-length human CXCR4 cDNA
Background Information	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). Chemicon's 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. Radiolabeled SDF-1a binds to the CXCR4 membranes with a Kd of 0.9 nM. With 0.04-0.13 nM 125I-labeled SDF-1a, an approximately 3-fold window of specific binding is obtained.

References

Product Information
Format	Membranes
Presentation	Packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA Packaging method: Membranes protein were adjusted to 0.5 mg/ml in 1 ml packaging buffer, rapidly frozen, and stored at -80°C.
Quality Level	MQ100

Applications
Application	Human CXCR4 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.
Key Applications	Radioligand binding assay GTPγS binding
Application Notes	Radioligand binding assay and GTPgammaS binding.

Biological Information
Concentration	2 mL, 0.5 mg/mL
Entrez Gene Number	NM_001008540.1 NM_003467.2
Entrez Gene Summary	This gene encodes a CXC chemokine receptor specific for stromal cell-derived factor-1. The protein has 7 transmembrane regions and is located on the cell surface. It acts with the CD4 protein to support HIV entry into cells and is also highly expressed in breast cancer cells. Mutations in this gene have been associated with WHIM (warts, hypogammaglobulinemia, infections, and myelokathexis) syndrome. Alternate transcriptional splice variants, encoding different isoforms, have been characterized.
Gene Symbol	CXCR4 WHIM NPY3R NPYY3R FB22 LAP3 Fusin CXCR-4 LCR1 NPYR HM89 fusin HSY3RR CXC-R4 NPYY3 NPYRL D2S201E CD184 LESTR
GPCR Class	A
Host Cells	Chem-1
Protein Target	CXCR4
Target Sub-Family	Chemokine
UniProt Number	P61073
UniProt Summary	FUNCTION: SwissProt: P61073 # Receptor for the C-X-C chemokine CXCL12/SDF-1. Transduces a signal by increasing the intracellular calcium ions level. Involved in haematopoiesis and in cardiac ventricular septum formation. Plays also an essential role in vascularization of the gastrointestinal tract, probably by regulating vascular branching and/or remodeling processes in endothelial cells. Could be involved in cerebellar development. In the CNS, could mediate hippocampal-neuron survival. Acts as a coreceptor (CD4 being the primary receptor) for HIV-1 X4 isolates and as a primary receptor for some HIV-2 isolates. Promotes Env-mediated fusion of the virus. SIZE: 352 amino acids; 39746 Da SUBUNIT: Interacts with HIV-1 surface protein gp120 and Tat. SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein. TISSUE SPECIFICITY: Expressed in numerous tissues, such as peripheral blood leukocytes, spleen, thymus, spinal cord, heart, placenta, lung, liver, skeletal muscle, kidney, pancreas, cerebellum, cerebral cortex and medulla (in microglia as well as in astrocytes), brain microvascular, coronary artery and umbilical cord endothelial cells. Isoform 1 is predominant in all tissues tested. DOMAIN: SwissProt: P61073 The amino-terminus is critical for ligand binding. Residues in all four extracellular regions contribute to HIV-1 coreceptor activity. PTM: Sulfated. DISEASE: SwissProt: P61073 # Defects in CXCR4 are a cause of WHIM syndrome [MIM:193670]; also called warts, hypogammaglobulinemia, infections, and myelokathexis. WHIM syndrome is an immunodeficiency disease characterized by neutropenia, hypogammaglobulinemia and extensive human papillomavirus (HPV) infection. Despite the peripheral neutropenia, bone marrow aspirates from affected individuals contain abundant mature myeloid cells, a condition termed myelokathexis. SIMILARITY: Belongs to the G-protein coupled receptor 1 family.
Incubation Conditions	RECOMMENDED ASSAY CONDITIONS: Membranes are mixed with radioactive ligand and unlabeled competitor (see Figures 1 and 2 for concentrations tested) in binding buffer in a nonbinding 96-well plate, and incubated for 1-2 h. Prior to filtration, a GF/C 96-well filter plate is coated with 0.33% polyethyleneimine for 30 min, then washed with 50 mM HEPES, pH 7.4, 0.5% BSA. Binding reaction is transferred to the filter plate, and washed 3 times (1 mL per well per wash) with Wash Buffer. The plate is dried and counted. Binding buffer: 50 mM Hepes, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.2% BSA, filtered and stored at 4°C Radioligand: [125I] SDF-1alpha (PerkinElmer#: NEX346) Wash Buffer: 50 mM Hepes, pH 7.4, 500 mM NaCl , 0.1% BSA, filtered and stored at 4°C. One vial contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 4-fold signal:background with ¹²⁵I-labeled SDF-1alpha at 0.13 nM.

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Table 1. Signal:background and specific binding values obtained in a competition binding assay with CXCR4 membrane prep, 0.13 nM ¹²⁵I-SDF-1α and a dilution series of unlabeled SDF-1α.

Product Usage Statements

	5 µg/well
Signal:Background	4.9
Specific Binding (cpm)	9004

Specifications:
1 unit = 5 μg
Bmax [¹²⁵I]-SDF-1alpha binding: 1.6 pmol/mg protein
Kd for [¹²⁵I] SDF-1alpha binding: ~ 0.9 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 Conditions	Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

Packaging Information
Material Size	200 units

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
Catalogue Number	GTIN
HTS004M	04053252285721

Documentation

Protocols

Title
Assembly of a Competition Binding Curve

ChemiSCREEN™ CXCR4 Membrane Preparation MSDS

Title
Safety Data Sheet (SDS)

ChemiSCREEN™ CXCR4 Membrane Preparation Certificates of Analysis

Title	Lot Number
ChemiscreenTM MEMBRANE PREPARATION HUMAN RECOMBINANT CXCR4 CHEMOKINE RECEPTOR - 2299342	2299342

References

Reference overview	Pub Med ID
HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Feng, Y, et al. Science, 272: 872-7 (1996) 1996 Show Abstract A cofactor for HIV-1 (human immunodeficiency virus-type 1) fusion and entry was identified with the use of a novel functional complementary DNA (cDNA) cloning strategy. This protein, designated "fusin," is a putative G protein-coupled receptor with seven transmembrane segments. Recombinant fusin enabled CD4-expressing nonhuman cell types to support HIV-1 Env-mediated cell fusion and HIV-1 infection. Antibodies to fusin blocked cell fusion and infection with normal CD4-positive human target cells. Fusin messenger RNA levels correlated with HIV-1 permissiveness in diverse human cell types. Fusin acted preferentially for T cell line-tropic isolates, in comparison to its activity with macrophagetropic HIV-1 isolates.	8629022

Reference overview

Pub Med ID

Brochure

Title
Product Selection Guide - Antibodies, small molecule inhibitors, kits, assays and proteins for signaling research.

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HTS004M Sigma-AldrichChemiSCREEN™ CXCR4 Membrane Preparation

Human CXCR4 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.

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