merck millipore,默克密理博,HTS004M,ChemiSCREEN™ CXCR4 Membrane Preparation

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merck millipore,默克密理博,HTS004M,ChemiSCREEN™ CXCR4 Membrane Preparation
产品名称：ChemiSCREEN™ CXCR4 Membrane Preparation
产品型号：HTS004M
Human CXCR4 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.

merck millipore,默克密理博,HTS004M,ChemiSCREEN™ CXCR4 Membrane Preparation

产品介绍

merck millipore,默克密理博,HTS004M,ChemiSCREEN™ CXCR4 Membrane Preparation

重要规格表

应用说明	品种	宿主细胞	蛋白靶
Radioligand binding assay and GTPgammaS binding.	Human	Chem-1	CXCR4

描述
产品目录编号	HTS004M
品牌系列	Chemicon®
商名	Chemicon ChemiScreen
描述	ChemiSCREEN™ CXCR4 Membrane Preparation
概述	Full-length human CXCR4 cDNA
背景信息	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.

产品信息
格式	Membranes
演示	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.

应用
应用	Human CXCR4 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.
应用说明	Radioligand binding assay and GTPgammaS binding.

生物信息
浓缩	2 mL, 0.5 mg/mL
品种	Human
品种反应性	Human
Entrez基因编号	NM_003467.2 NM_001008540.1
Entrez基因汇总	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.
基因符号	LESTR CXCR4 WHIM NPY3R NPYY3R FB22 LAP3 Fusin CXCR-4 LCR1 NPYR HM89 fusin HSY3RR CXC-R4 NPYY3 NPYRL D2S201E CD184
GPCR类别	A
宿主细胞	Chem-1
蛋白靶	CXCR4
靶子系列	Chemokine
UniProt编号	P61073
UniProt汇总	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.
孵化条件	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.

产品使用声明

质量保证

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.

	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

使用声明

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.