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. 2013 Nov 25;110(50):20224–20229. doi: 10.1073/pnas.1314239110

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Fig. 1. — Biochemical and cellular activities of LGK974. (A) PORCN identified as the target of Wnt secretion inhibitor, GNF-1331. [³H]-GNF-1331 binds to the membrane preps made from PORCN-transfected 293T cells but not from Wntless or vector control-transfected 293T cells. The binding signals could be competed off by 70-fold unlabeled GNF-1331. (B) The structure of LGK974. (C) LGK974 interacts with PORCN. LGK974 competes off [³H]-GNF-1331 in a dose-dependent manner. (D) LGK974 inhibits Wnt signaling reporter assay with an IC₅₀ of 0.4 nM. (E) The cellular activities of LGK974 were rescued in the presence of Wnt3A CM. (F) LGK974 strongly inhibited Wnt secretion in 293A cells transfected with human HA-Wnt3A.