WZ811

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).¹ 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).¹ The effectiveness of WZ811 in animals remains to be elucidated.

WARNING This product is not for human or veterinary use.

1. Zhan, W., Liang, Z., Zhu, A., et al. Discovery of small molecule CXCR4 antagonists. J. Med. Chem. 50, 5655-5664 (2007).