Free shipping on all orders over $ 500

LGK-974

Cat. No. M2812
LGK-974 Structure
Size Price Availability Quantity
1mg USD 54  USD60 In stock
5mg USD 108  USD120 In stock
10mg USD 189  USD210 In stock
50mg USD 576  USD640 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

LGK-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
Protocol
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 59 mg/mL
Storage at -20°C
References

Differentiation of mesenchymal stem cells into cardiomyocytes is regulated by miRNA-1-2 via WNT signaling pathway.
Shen X, et al. J Biomed Sci. 2017 May 10;24(1):29. PMID: 28490365.

Wnt inhibition induces persistent increases in intrinsic stiffness of human trabecular meshwork cells.
Morgan JT, et al. Exp Eye Res. 2015 Mar;132:174-8. PMID: 25639201.

Related Wnt/beta-catenin Products
FIDAS-5

FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM.

BML-284

BML-284 (Wnt agonist 1) is a potent and selective activator of Wnt signaling.

SKL2001

SKL2001 is a novel agonist of Wnt/β-catenin pathway with anti-cancer activity.

Adavivint

Adavivint (SM04690) is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter.

Gallocyanine

Gallocyanine is a small molecule DKK1 inhibitor, which blocks DKK1 inhibitory activity on Wnt signaling.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LGK-974 supplier, Wnt/beta-catenin, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.