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. Author manuscript; available in PMC: 2016 Dec 28.
Published in final edited form as: Cell Stem Cells Regen Med. 2016 May 30;2(2):10.16966/2472-6990.111. doi: 10.16966/2472-6990.111

Figure 1. GNF-6231 inhibits canonical WNT pathway activity in vitro.

Figure 1

(A) Schematic of the WNT pathway and point of action of WNT inhibitors, GNF-6231 and C-113. (B) Fold change in Axin2 gene expression in WNT3a overexpressing cardiac cells showing GNF-6231 treatment reduced WNT target gene expression (N=3 replicates from independent experiments; ***p ≤ 0.0001; Repeated measures ANOVA with Bonferroni correction for multiple comparisons). (C) IV free plasma level of GNF-6231 after a single intravenous injection of 5 mg/kg. The plasma half-life of the drug was approximately 2.3 hours; GNF-6231 free plasma concentrations were above the in vitro Porcupine IC50 for >12 h. (D) qRT-PCR showed inhibition of Axin2 gene expression in liver at different time points following a single 5 mg/kg intravenous treatment with GNF-6231 (N=2 mice per timepoint). Bars represent Mean ± SD.