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Description: WZ811 (WZ-811; WZ 811) is a highly potent, selective, competitive antagonist of CXCR4 chemokine receptor with potential anticancer activity. It inhibits CXCR4with subnanomolar potency (EC50 = 0.3 nM) in an affinity binding assay. WZ811 efficiently inhibits CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cyclic adenosine monophophate (cAMP) levels (EC50 = 1.2 nM) and SDF-1 induced Matrigel invasion (EC50 = 5.2 nM).
References: J Med Chem. 2007 Nov 15;50(23):5655-64.
Product Catalog 2022
Guide to Product Handling
Chemical Name: N,N'-(1,4-phenylenebis(methylene))bis(pyridin-2-amine)
InChi Key: KBVFRXIGQQRMEF-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H18N4/c1-3-11-19-17(5-1)21-13-15-7-9-16(10-8-15)14-22-18-6-2-4-12-20-18/h1-12H,13-14H2,(H,19,21)(H,20,22)
SMILES Code: C1(CNC2=NC=CC=C2)=CC=C(CNC3=NC=CC=C3)C=C1
WZ811; WZ-811; WZ 811
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro 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.
Cell Assay: 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.
J Med Chem. 2007 Nov 15;50(23):5655-64.
Purity ≥98%
COA
MSDS