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

Figure 1

NCI8642 is able to abolish DKK1-LRP6 interaction at the cell surface. (A) Immunostaining of DKK1 on HEK293 cells (panel a), on HEK293-LRP6 cells (panel b), on HEK293-LRP6 cells in the presence of 1% DMSO (panel c), and on HEK293-LRP6 cells in the presence of 100 μM NCI8642 (panel d). Immunostaining of AP-DKK1 on HEK293-LRP6 cells (panel e and f). The cell-bound DKK1 was detected with anti-DKK1 antibody. (B) Enzymatic quantification of AP-DKK1 binding to HEK293-LRP6 cells, in the presence of increasing concentrations of NCI8642.