Human CXCR4 Stable Cell Line - U2OS

C-X-C Motif Chemokine Receptor 4 (CXCR4) is a highly conserved G protein-coupled receptor that plays an indispensable role in numerous biological processes within the human body. Unlike many chemokine receptors capable of binding to multiple ligands, CXCR4 exhibits high specificity, primarily binding to a single chemokine ligand: stromal cell-derived factor-1 (SDF-1), also known as CXCL12. The signaling axis formed by CXCR4 and CXCL12 plays a foundational role in embryonic development, hematopoiesis, angiogenesis, as well as the mobilization and directed migration of immune cells. Upon ligand binding, CXCR4 triggers a diverse array of intracellular signaling cascades, thereby regulating cellular survival, proliferation, and chemotactic behavior. In addition to its critical physiological functions, the CXCR4 gene is also closely implicated in various severe pathological conditions. The gene first garnered widespread attention within the global scientific community when it was identified as one of the primary co-receptors (acting in concert with the CD4 receptor) utilized by the Human Immunodeficiency Virus (HIV) to invade target T lymphocytes. Furthermore, aberrant expression of the CXCR4 gene is strongly associated with the progression and metastasis of various types of cancer, including breast, lung, prostate, and ovarian cancers.

The human CXCR4 stable cell line—U-2 OS—was generated by transfecting an expression vector carrying the full-length human CXCR4 gene into the U-2 OS human osteosarcoma cell line. This process yielded a robust cell population capable of consistently and stably expressing high levels of the CXCR4 receptor on the cell surface. The selection of the U-2 OS cell line as the cellular background offers significant advantages: this cell line exhibits excellent adherence properties, is easy to culture, and provides a clean cellular environment—an environment highly conducive to conducting various functional assays while remaining largely free from significant interference by endogenous background signals. Researchers widely utilize these cells to screen for and identify potential CXCR4 antagonists, inverse agonists, and allosteric modulators—steps that are critical within drug development pipelines targeting HIV entry inhibitors and anticancer therapies. Furthermore, this cell line has been optimized for use in a wide range of cell-based assays, including intracellular calcium mobilization assays, beta-arrestin recruitment assays, radioligand binding studies, and receptor internalization imaging analyses.