CXCR4 Assay(s)

Background Information

Gi-coupled chemokine receptor mediating hematopoietic stem cell (HSC) homing to bone marrow, immune cell trafficking, and tumor metastasis. CXCR4 antagonism disrupts HSC retention in bone marrow for stem cell mobilization. C-terminal GoF mutations cause WHIM syndrome. Tumor cells exploit CXCL12/CXCR4 signaling for metastasis to lymph nodes, bone marrow, and lungs.

Family: GPCR
Protein Name: CXCR4
Gene Name: CXCR4

Organism: Human
Therapeutic Area: Immunology, Oncology, Rare-disease

Assay Information

Validated Assay(s): cAMP, Calcium Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: Panoptic
Plate Format: 384-well
Expression: Transient
Cell type: HEK293T

Testing Information

Functional Mode(s): Agonist
Reference compound(s): CXCL12, CTCE-0214

CTCE-0214 concentration-response curve for the human CXCR4 receptor in a fluorescence-based GPCR assay using HEK293T cells.
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