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WZ811 55778-02-4

Product Description

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Molecular Weight:

290.36 WZ811 is a highly potent Competitive CXCR4 Antagonist with EC50 of 0.3 nM.

Biological Activity

WZ811 is a highly potent competitive antagonist of CXCR4. WZ811 is
effective in counteracting SDF-1 on cAMP reduction at doses as low as a
few nanomoles. WZ811 blocks SDF-1-mediated invasion with EC50 of 5.2 nM.

Binding affinity

For compound screening based on a competition binding assay, 2 × 104 MDA-MB-231 cells in 200μL of medium are seeded in an 8-well slide
chamber 2 days before the experiments. Various concentrations of WZ811
(1, 10, 100, and 1000 nM) are added to the separate wells and incubated
for 10 min at room temperature, and then the cells are fixed in 4%
ice-cold paraformaldehyde.


The cells are rehydrated in
phosphate-buffered saline (PBS) and blocked to eliminate nonspecific
binding. The slides are subsequently incubated for 45 min at room
temperature with 0.05 μg/mL biotinylated 3, washed three times with PBS,
and incubated in streptavidin-rhodamine (1:150 dilution) for 30 min at
room temperature. Finally, the slides are washed with PBS and mounted in
an antifade mounting solution.



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Product Categories : GPCR & G Protein > CXCR Inhibitor