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Competitive CXCR4 antagonist,highly potent
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WZ811 is a small molecule antagonist of CXC chemokine receptor 4 (CXCR4) [1].

WZ811 is synthesized with two aromatic amine moieties. It is found to effectively inhibit TN14003 binding to CXCR4 with EC50 value of 0.3nM at first. And then WZ811 is found to have ability in counteracting SDF-1 function and blocking CXCR4/SDF-1-mediated signaling. In the cAMP assay, WZ811 reduces the effect on cAMP caused by 150ng/ml SDF-1 significantly. It also blocks the SDF-1 induced Matrigel invasion with EC50 value of 5.2nM. Since CXCR4 is involved in the pathogeneses of a wide range of infectious, inflammatory and other diseases, WZ811 is developed for the treatment of various CXCR4-related diseases. It is reported to have weak anti-HIV activity in cell culture [1, 2].

[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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
Cas No.55778-02-4
SolubilitySoluble in DMSO
Chemical NameN-[[4-[(pyridin-2-ylamino)methyl]phenyl]methyl]pyridin-2-amine
SDFDownload SDF
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description WZ811 is a highly potent competitive antagonist of CXCR4 with an EC50 value of 0.3 nM.
Targets CXCR4          
IC50 0.3 nM(EC50)          

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