PathHunter® Human CXCR4 Total GPCR Internalization Cell-Based Assay Kit (U2OS)

Background Information:

The PathHunter® Human CXCR4 Total GPCR Internalization Cell-Based Assay Kit (U2OS) utilizes the CXCR4 Total GPCR internalization cell line. The stable engineered cell line is for use in studying drug candidates (small molecules or biologics) affecting GPCR activation and internalization. This cell line enables assessment of ligand (e.g. CXCL12/SDF-1α) based internalization of CXCR4 via detection of localization to the early endosome. This product uses EFC technology. The included cell line overexpresses PK-tagged CXCR4 and an EA-tagged early endosome protein. Upon ligand-induced receptor activation, the resulting internalization of the CXCR4 receptor to the early endosome leads to production of the EFC signal. This product leverages a sensitive chemiluminescent detection system that delivers a wide dynamic range and robust Z’ for potency, efficacy, and rank‑order profiling across small molecules and biologics.
This kit includes a stable engineered cell line (supplied as two vials of cryopreserved cells); cell line specific reagents for cell thawing, propagation, detachment, cryopreservation, and cell plating; and a 10‑plate detection kit required to run the assay. Assay plates and positive control for use in the assays can be purchased separately. For continued use of the cell line, additional quantities of cell culture and assay reagents are available for purchase separately.
Eurofins DiscoverX optimized Detection Reagents are required for optimal assay performance and must be used with these cell lines in accordance with the cell line license agreed to upon purchase of this cell line assay kit.

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