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Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM.
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Source | Stem Cells Transl Med (2016). Figure 4. Wnt-C59 |
| Method | qPCR | |
| Cell Lines | human iPSCs | |
| Concentrations | 10 nM | |
| Incubation Time | 4 or 5 days | |
| Results | qPCR analyses revealed that neural aggregates differentiated with C59 contained more cells with rostral identity compared with DKK1 or XAV |
| Cell Experiment | |
|---|---|
| Cell lines | NMuMG (NMG) and MDA-MB 231 cells |
| Preparation method | Cells are seeded at a concentration of 4×103/well in 100 μL culture medium containing various amouts of Wnt-C59 and incubated for 48 hours at 37 ℃. Add 10 μL/well cell proliferation reagent and incubate for 4 hours at 37 ℃. Shake thoroughly for 1 min on a shaker. Measure the absorbance of the samples in a microplate (ELISA) reader. |
| Concentrations | |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors |
| Formulation | 0.5% methylcellulose and 0.1% Tween-80 |
| Dosages | 10 mg/kg |
| Administration | orally |
| Molecular Weight | 379.45 |
| Formula | C25H21N3O |
| CAS Number | 1243243-89-1 |
| Solubility (25°C) | DMSO 56 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Wnt/beta-catenin Products |
|---|
| XAV939
XAV939 is a potent, cell-permeable small molecule inhibitor of the Wnt/β-catenin pathway to TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively. |
| ICG-001
ICG-001 is a novel small molecule inhibitor of TCF/beta-catenin-mediated transcription. ICG-001 specifically binds to cyclic AMP response element-binding protein with an IC50 of 3 μM. |
| IWP-2
IWP-2 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 27 nM. |
| IWP-L6
IWP-L6 is a highly potent Porcn inhibitor with EC50 of 0.5 nM. |
| IWR-1-endo
IWR-1 (endo-IWR 1) is a Wnt pathway inhibitor with IC50 of 180 nM, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. |
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