The CXC chemokine receptor-4 (CXCR4) is a G protein-coupled receptor that is specific for stromal cell-derived factor-1 (SDF-1/ CXCL12). Activation of CXCR4 promotes homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Moreover, CXCR4 on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. WZ811 is a potent inhibitor of binding of an SDF-1 peptide mimic to CXCR4 (EC50 = 0.3 nM). It prevents SDF-1/CXCL12-mediated modulation of cAMP (EC50 = 1.2 nM) in cells and blocks SDF-1-induced Matrigel™ invasion by MDA-MB-231 human breast adenocarcinoma cells (EC50 = 5.2 nM). The effectiveness of WZ811 in animals remains to be elucidated.
N1,N4-di-2-Pyridinyl-1,4-benzenedimethanamine acts as an inhibitor for the chemokine receptor CXCR4.
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