Biological Information
Background Information:
CXCR4 (CXC Chemokine Receptor 4), also called fusin, is an alpha-chemokine receptor specific for stromal-derived-factor-1 (SDF-1 also called CXCL12), a molecule endowed with potent chemotactic activity for lymphocytes. It is highly expressed in brain and heart, and in white blood cells, vascular endothelial cells, umbilical cord endothelial cells, and several tumor cell lineages. This receptor is an HIV-1 fusion co-factor that allows HIV-1 invasion in diverse human cell types. CXCR4 is involved in organ vascularization, neuronal cell migration, and patterning of the central nervous system during development.
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.
Family:
GPCR
Sub Family:
Chemokine
Class:
Class A
Coupling:
Gi/Go
Protein Name:
CXCR4
Uniprot Number:
P70658
Protein Aliases:
CXCR-4|Fusin|Leukocyte-derived seven transmembrane domain receptor|LESTR|Pre-B-cell-derived chemokine receptor|PB-CKR|Stromal cell-derived factor 1 receptor|SDF-1 receptor|CD antigen CD184
Gene Name:
CXCR4
Gene ID:
12767
Gene Aliases:
LESTR|NPY3R|HM89|NPYY3R|D2S201E|fusin|HSY3RR|NPYR|CD184
Accession Number:
NM_009911.2
Organism:
Mouse
Cell Type:
U2OS
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
β-Arrestin Isoform:
β-Arrestin-2
Testing Information
Control Activator:
mCXCL12/SDF-1a
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 10 concentrations are selected
Test Sample Requirements:
40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)
Minimum Order Quantity:
20
Turnaround Time
Standard:
15 Business Days
Clinical Relevance
Adverse / Beneficial Action:
CXCR4 antagonists may be useful for the treatment of AIDS, tumors and inflammatory diseases.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA