All AbMole products are for research use only, cannot be used for human consumption.
LGK-974 (WNT-974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.
 |
Source | Nat Med (2015). Figure 5. LGK-974 |
| Method | Western blot | |
| Cell Lines | MCF-7 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 48 h | |
| Results | LGK-974 (1 μM), an inhibitor of Wnt ligands, decreased fentanyl-activated b-catenin, p-GSK-3b (Ser9) and FUT8 expression |
| Cell Experiment | |
|---|---|
| Cell lines | HPAF-II, PaTu 8988S, and Capan-2 cells |
| Preparation method | Cells are plated in growth medium in a 96-well plate at a density of 6,000–12,000 cells per well and treated with DMSO or 1 μM LGK974. After 3 d, the cells are treated with fresh growth medium containing 20 μM EdU, which is included in the Click-iT EdU Alexa Fluor 488 HCS assay kit, and the plate was incubated for 2 h at 37 °C in a humidified atmosphere containing 5% CO2. Cells are fixed with final 4% (mass/vol) paraformaldehyde for 30 min, washed with PBS, permeabilized, and stained with 50 μg/mL Hoechst in PBS for 30 min. After wash, the cells are proceeded to EdU detection according to the instruction of Click-iT EdU assay kit. Triplet wells are performed for each condition. |
| Concentrations | ~1 μM |
| Incubation time | 3 d |
| Animal Experiment | |
|---|---|
| Animal models | A murine MMTV-Wnt1 tumor model and a human head and neck squamous cell carcinoma model (HN30) |
| Formulation | 10% (vol/vol) citrate buffer (pH 2.8)/90% (vol/vol) citrate buffer (pH 3.0) or 0.5% MC/0.5% Tween 80 |
| Dosages | ~3 mg/kg daily |
| Administration | Oral gavage |
| Molecular Weight | 396.44 |
| Formula | C23H20N6O |
| CAS Number | 1243244-14-5 |
| Solubility (25°C) | DMSO 30 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
