TABLE 2 

Interventions in WNT synthesis and secretion

InterventionUseProposed TargetEffectAffinityReference
Porcn genetic deletionIn vivo (mice)Porcn geneInhibition of WNT3A secretionn/aBarrott et al. (2011)
IWP-1In vitroPORCN proteinInhibition of WNT secretion (WNT1, -2, and -3A?)IC50: 58 nMChen et al. (2009a)
IWP-2In vitroPORCN proteinInhibition of WNT-1, -2, −3a secretionIC50: 27 nMChen et al. (2009a)
IWP-3In vitroPORCN proteinInhibition of WNT secretion (WNT1, -2, and -3A?)IC50: 40 nMChen et al. (2009a)
IWP-4In vitroPORCN proteinInhibition of WNT secretion (WNT1, -2, and -3A?)IC50: 25 nMChen et al. (2009a)
IWP-L6In vitroPORCN proteinInhibition of WNT secretionIC50: 0.5 nMWang et al. (2013b)
LGK974In vitroPORCN proteinInhibition of WNT1, -2, -3, -3A, −6, -7A, and -9A secretionIC50: 0.3–0.4 nM (depending on the cell assay)Liu et al. (2013)
ETC-159In vitroPORCN proteinInhibition of WNT1, -2, -3A, -6, -7B, −8A, -9A, -9B, and -10B secretionIC50: 2.9 nM β-catenin reporter assay)Madan et al. (2016a)
IC50: 18.1 nM (mouse PORCN inhibition)
WNT-C59In vitro and in vivo (mice)PORCN proteinInhibition of WNT1, -2, -3A, -6, -7B, −8A, -9A, -9B, and -10B secretionIC50: 74 pM (WNT-3a-mediatedProffitt et al. (2013)
TOPFLASH assay)
Compound 53In vitroPORCN proteinInhibition of WNT-3a secretionIC50: 0.5 nMXu et al. (2016)
4,4-DiOMEAIn vitroPORCN protein?Inhibition of WNT-16 secretionIC50: 7.6 ± 1.5 nMRamirez de Molina et al. (2015)