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Cat. No. M2812
LGK-974 Structure

WNT974; NVP-LGK974

Size Price Availability Quantity
2mg USD 75  USD75 In stock
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
50mg USD 620  USD620 In stock
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Quality Control
Biological Activity

LGK-974 (WNT-974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.

Customer Product Validations & Biological Datas
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 396.44
Formula C23H20N6O
CAS Number 1243244-14-5
Purity 99.29%
Solubility DMSO 30 mg/mL
Storage at -20°C

[1] Shen X, et al. J Biomed Sci. Differentiation of mesenchymal stem cells into cardiomyocytes is regulated by miRNA-1-2 via WNT signaling pathway.

[2] Morgan JT, et al. Exp Eye Res. Wnt inhibition induces persistent increases in intrinsic stiffness of human trabecular meshwork cells.

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Keywords: LGK-974, WNT974; NVP-LGK974 supplier, Wnt/beta-catenin, inhibitors

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