OMP-18R5 (mAb) | In vitro and in vivo (mice) | FZD1, FZD2, FZD5, FZD7, FZD8 | Inhibition of WNT-FZD interaction | n/a | Gurney et al. (2012) |
OTSA101 (mAb) + Yttrium 90 | In vitro, in vivo (mice) and CT | FZD10 | Inhibition of WNT-FZD interaction | n/a | Fukukawa et al. (2008) |
TT641 (pAb) | In vitro and in vivo (mice) | FZD10 | Inhibition of WNT-FZD interaction | n/a | Nagayama et al. (2005) |
1.99.15 (mAb) | In vitro and in vivo (mice) | FZD4 | Inhibition of WNT-FZD interaction | n/a | Paes et al. (2011) |
pAb against FZD5 | In vitro | FZD5 | Inhibition of WNT-FZD interaction | n/a | Sen et al. (2001) |
Ab against FZD7 | In vitro and in vivo (chick embryo) | FZD7 | Inhibition of WNT-FZD interaction | n/a | Pode-Shakked et al. (2011) |
OMP-54F28 fusion protein | In vitro, in vivo (mice) and CT | FZD8-interacting WNT ligands | Inhibition of WNT-FZD interaction | n/a | Le et al. (2015), Fischer et al. (2015) |
| | | | Jimeno et al. (2014) |
UM206 | In vitro and in vivo (mice) | FZD1 and FZD2 | Inhibition of WNT-FZD interaction | IC50: 2.10 nM for rFZD1; | Laeremans et al. (2011) |
| | | | IC50: 0.0169 nM for rFZD2 | Uitterdijk et al. (2016) |
Foxy5 + FZD5 receptor-blocking Ab | In vitro and in vivo (mice) | FZD5 | Mimicking of WNT5A (effect independent of β-catenin) | n/a | Safholm et al. (2006)Safholm et al. (2008) |
Box5 | In vitro | FZD5 (?) | Blockade of WNT5A signaling | n/a | Jenei et al. (2009) |
3235–0367 | In vitro | FZD8 CRD | Inhibition of WNT-FZD interaction | IC50: 7.1 μM | Lee et al. (2015) |
1094–0205 | In vitro | FZD8 CRD | Inhibition of WNT-FZD interaction | IC50: 5 μM | Lee et al. (2015) |
2124–0331 | In vitro | FZD8 CRD | Inhibition of WNT-FZD interaction | IC50: 10.4 μM | Lee et al. (2015) |
NSC36784 | In vitro | FZD8 CRD | Inhibition of WNT-FZD interaction | IC50: 6.5 μM | Lee et al. (2015) |
NSC654259 | In vitro | FZD8 CRD | Inhibition of WNT-FZD interaction | IC50: 5.7 μM | Lee et al. (2015) |
Niclosamide | In vitro | FZD1 (internalization) | Inhibition of WNT-FZD interaction | IC50: 0.5 μM | Chen et al. (2009b) |
| In vitro | LRP6 | LRP6 degradation | IC50: 0.33–0.75 μM | Lu et al. (2011b) |
| | | | (depending on the cell line) | |
Curcumin | In vitro | FZD1 | Inhibition of WNT-FZD interaction (?) | n/a | Yan et al. (2005) |
| In vitro | WNT3A; LRP6 | Inhibition of WNT-FZD interaction (?) | n/a | Zheng et al. (2017) |
| In vitro | WNT10B; FZD2; LRP5 | Enhancement of WNT-FZD interaction | n/a | Ahn et al. (2010) |
anti-Sclerostin Ab | In vitro | Sclerostin binding | Prevention of Sclerostin-mediated disruption | n/a | van Dinther et al. (2013) |
| | to LRP5/6 | of LRP5/6-FZD complex formation | | |
Salinomycin | In vitro | LRP6 (?) | Inhibition of WNT1/FZD5/LRP6 and | IC50: 163 nM (WNT-1) | Lu et al. (2011) |
| | | WNT3/FZD5/LRP6 complexes | | |
| In vitro | LRP6 | Inhibition of WNT/FZD/LRP6 complex (?) | n/a | Lu and Li (2014) |
Leptin | In vivo (mice) | LRP6; WNT4 and WNT7 (?); | Enhancement of WNT4/FZD/LRP6 | n/a | Benzler et al. (2013) |
| | GSK-3β | and WNT7A/FZD/LRP6 complexes | | |
Silibinin | In vitro | LRP6 | Inhibition of WNT3A/FZD/LRP6 complex | IC50: 34–122 μM (depending on the cell line) | Lu et al. (2012) |
anti-LRP6 Abs | In vitro | LRP6 | Inhibition of WNT1 and WNT3A-mediated cascade | n/a | Ettenberg et al. (2010) |
| | | (WNT/FZD/LRP6 complex?) | | |
| In vitro | LRP6 | Inhibition or enhancement of WNT1/2/2B/4/6/7A/7B/8A/9B/10A/10B-mediated | n/a | Gong et al. (2010) |
| | | cascade (WNT/FZD/LRP6 complex?) | | |
28aa peptide | In vitro andin vivo (mice) | LRP5/6 | Mimicking of LRP5/6-domain → Enhancement of | n/a | Hay et al. (2012) |
| | | WNT signaling (via N-cadherin) | | |
DKK1 and DKK2 | In vivo (Xenopus embryos) | LRP6 | Inhibition of WNT signaling | n/a | Mao et al. (2001) |
anti-DKK1 Ab | In vitro and in vivo (mice) | DKK1 | Neutralization of DKK1 → Enhancement of WNT signaling | n/a | Sato et al. (2010b) |
| | | | | |
BHQ880 mAb | In vitro, in vivo (mice) and CT | DKK1 | Neutralization of DKK1 → Enhancement of WNT signaling | n/a | Fulciniti et al. (2009) |
| | | | | Iyer et al. (2014) |
DKK1 vaccine | In vivo (mice) | DKK1 | Enhancement of DKK1 levels → Inhibition of WNT signaling | n/a | Qian et al. (2012) |
Iminooxothiazolidines (Compounds 1–34) | In vitro | sFRP1 | Inhibition of sFRP1 → Enhancement of WNT signaling | EC50: 7.2 μM (Compound 1) | Shi et al. (2009) |
WAY-316606 | In vitro | sFRP1 | Inhibition of sFRP1 → Enhancement of WNT signaling | IC50: 0.5 μM | Bodine et al. (2009) |
| | | | EC50: 0.65 μM | Moore et al. (2010) |
N-substituted piperidinyl | In vitro | sFRP1 | Inhibition of sFRP1 → Enhancement of WNT signaling | IC50: 0.04–0.87 μM | Moore et al. (2010) |
diphenylsulfonyl sulfonamides | | | | ED50: 0.07–1.9 μM | |