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