BML-286 (Compound 3289-8625) is a small molecule inhibitor of the PDZ domain of dishevelled (Dvl) with KD of 10.6 uM, competitively inhibits the Wnt signaling.
Compound 3289-8625 (3 uM) inhibits Wnt signaling, effectively reduces luciferase activity by about 2-fold 293 cell line stably transfected with a luciferase reporter.
Compound 3289-8625 is cell-permeable and 3289-8625 (10 uM) blocks Wnt signaling in Xenopus, inhibits Wnt pathway responses in culture and in vivo.
Compound 3289-8625 suppresses cell proliferation and reduces β-catenin level in prostate cancer PC-3 cells, decreases the levels of β-catenin in both cytosolic fraction and membrane fraction.
Compound 3289-8625 sensitized A2780/Taxol cells to paclitaxel.
Physicochemical Properties
M.Wt
374.40
Formula
C22H18N2O4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
2-(3-(2-phenylacetamido)benzamido)benzoic acid
References
1. David Grandy, et al. J Biol Chem. 2009 Jun 12;284(24):16256-16263.
