BML-286 is a cell-permeable compound whose binding of the PDZ domain of dishevelled (Kd = 10.6 µM) disrupts Wnt signaling. Further, BML-286 blocked Wnt3a-induced transcription activity and was able to suppress the Wnt pathway-dependent growth of prostate cancer PC-3 cells in vitro (IC50 = 12.5 µM).
1. Grandy, David., et al., 2009. Discovery and characterization of a small molecule inhibitor of the PDZ domain of dishevelled. The Journal of biological chemistry. 284(24): 16256-63. PMID: 19383605
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