Product Details
| Product Name:
LGK974 |
CAS No.:
1243244-14-5 |
| Purity:
≥98% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | LGK974 |
| Description | LGK974 (NVP-LGK974) is an effective and selective PORCN inhibitor and inhibits Wnt signaling (IC50: 0.4 nM) in TM3 cells. It has been used in trials studying the treatment of Metastatic Colorectal Cancer and Squamous Cell Carcinoma, Head And Neck. |
| Cell Research | 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 humidi?ed atmosphere containing 5% CO2. Cells are ?xed with ?nal 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. (Only for Reference) |
| Kinase Assay | Radioligand binding assay: using the aforementioned membrane preps, filtration binding assays are performed. To reduce nonspecific binding, 96-well filtration plates are precoated as suggested by the manufacturer with 0.1% BSA and then washed four times with 0.1% BSA. Membrane preps (50 μg total protein) are incubated in polypropylene 96-well plates with 6.6 nM 3H-GNF-1331 in the presence or absence of a testing compound in binding buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 0.1% BSA) plus EDTA-free protease inhibitor mixture in a final volume of 150 μL for 3 h at room temperature. Binding reaction mixtures are then transferred to the precoated 96-well filtration plates, filtered, and washed using a 96-pin FilterMate Harvester. Radioactive signals are obtained using a Microplate Scintillation Counter TopCount. Curve fitting is performed using Prism[1]. |
| In vitro | In both the MMTV-WNT1 mouse model of breast carcinoma and the human head and neck squamous cell carcinoma model (hn30), LGK-974 (3 mg/kg) inhibits the Wnt signaling pathway, leading to tumor regression without affecting mouse body weight. Additionally, LGK-974 (5 mg/kg, twice daily, orally) also suppresses the growth of RNF43-mutant pancreatic tumors (HPAF-II and Capan-2). |
| In vivo | LGK-974 inhibits a range of tested Wnts, with IC50 values between 0.05 to 2.4 nM. In the PORCN radioligand binding assay, LGK-974 effectively displaces [3H]GNF-1331 with an IC50 of 1 nM and exhibits minimal cytotoxicity at 20 μM. It specifically inhibits the growth of RNF43 mutant cell lines HPAF-II, PaTu 8988S, and Capan-2. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 73 mg/mL (184.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
|
| Keywords | WNT-974 | WNT 974 | Porcupine | NVP-LGK-974 | NVP-LGK 974 | LGK974 | Inhibitor | inhibit |
| Inhibitors Related | IWP L6 | Porcn-IN-1 | ETC-159 | GNF-6231 | WHN-88 | IWP-2 | Wnt-C59 | IWP-O1 |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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