Functional Characterization of a Small-Molecule Inhibitor of the DKK1-LRP6 Interaction

<table>NCI8642 is able to compete with DKK1 in <i>β</i>-catenin translocation assay. (A) Panel a: Wnt3a-stimulated cells; panel b: cells treated with Wnt3a and DKK1; panel c: cells treated with Wnt3a, DKK1, and 50 <i>μ</i>M NCI8642; panel d: cells treated with 50 <i>μ</i>M NCI8642 only. (B) Concentration-response curve of NCI8642 (from 1 to 50 <i>μ</i>M) expressed as % of activity. The activity was defined as the ratio of nuclear/cytoplasmic intensity normalized between Wnt3a + DMSO treatment (100% activity) and Wnt3a + DKK1 + DMSO treatment (0% activity).</table>

International Scholarly Research Notices

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Figure 5

Figure 5: Functional Characterization of a Small-Molecule Inhibitor of the DKK1-LRP6 Interaction 