N1,N4-Di-2-pyridinyl-1,4-benzenedimethanamine

Description

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.

Uses

N1,N4-di-2-Pyridinyl-1,4-benzenedimethanamine acts as an inhibitor for the chemokine receptor CXCR4.

in vivo

IC 50

CXCR4: 0.3 nM (EC₅₀)

References

[1] zhan w, liang z, zhu a, et al. discovery of small molecule cxcr4 antagonists. journal of medicinal chemistry, 2007, 50(23): 5655-5664.
[2] choi w t, duggineni s, xu y, et al. drug discovery research targeting the cxc chemokine receptor 4 (cxcr4). journal of medicinal chemistry, 2011, 55(3): 977-994.