PathHunter® CXCR4 Total GPCR Internalization U2OS Cell Line

Background Information:

The PathHunter® CXCR4 Total GPCR Internalization Cell Line is a stable, engineered cell line designed to study drug candidates (small molecules or biologics) that affect GPCR activation and internalization. This cell line enables the assessment of ligand-induced internalization of CXCR4, for example, in response to CXCL12/SDF-1α. The assay is based on Enzyme Fragment Complementation (EFC) technology. The cell line overexpresses a PK-tagged CXCR4 receptor and an Enzyme Acceptor (EA) tag localized to the plasma membrane, enabling complementation of the two β-galactosidase enzyme fragments (EA and PK). Upon ligand-induced receptor activation, CXCR4 undergoes internalization, disrupting EA/PK complementation and resulting in a loss of chemiluminescent signal.
This stable engineered cell line is provided as two vials of cryopreserved cells.

Target Class:

GPCR

Family:

Chemokine

Sub Family:

Class A

Coupling:

Gi/Go

Protein Name:

CXCR4

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

Accession Number:

AY242129

UniProt Number:

P61073

Gene Name:

CXCR4

Gene ID:

7852

Gene Aliases:

LESTR|NPY3R|HM89|NPYY3R|D2S201E|fusin|HSY3RR|NPYR|CD184

Target Species:

Human

Cell Background:

U2OS