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LGK974

Catalog No. T2618   CAS 1243244-14-5
Synonyms: LGK 974, LGK-974, NVP-LGK974, WNT974

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
LGK974 Chemical Structure
LGK974, CAS 1243244-14-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 97.00
10 mg In stock $ 167.00
25 mg In stock $ 319.00
50 mg In stock $ 573.00
100 mg In stock $ 819.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 100%
Purity: 99.79%
Purity: 99.34%
Purity: 99.16%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 Porcn:0.4 nM
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].
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)
Synonyms LGK 974, LGK-974, NVP-LGK974, WNT974
Molecular Weight 396.44
Formula C23H20N6O
CAS No. 1243244-14-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 73 mg/mL (184.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Liu J, et al. Proc Natl Acad Sci U S A. 2013, 110(50), 20224-20229. 2. Jiang X, et al. Proc Natl Acad Sci U S A. 2013, 110(31), 12649-12654.

TargetMolCitations

1. Zhang W, Li X, Jiang M, et al.SOCS3 deficiency-dependent autophagy repression promote the survival of early-stage myeloid-derived suppressor cells in breast cancer by activating the Wnt/mTOR pathway.Journal of Leukocyte Biology.2023: qiad020.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compound Library Anti-Colorectal Cancer Compound Library NO PAINS Compound Library Anti-Aging Compound Library Wnt/Hedgehog/Notch Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets
ETC-159 Porcn-IN-1 GNF-6231 IWP L6 IWP-2 Wnt-C59 IWP-O1

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Keywords

LGK974 1243244-14-5 Stem Cells Porcupine LGK 974 NVP-LGK 974 LGK-974 Inhibitor WNT 974 WNT-974 NVP-LGK974 inhibit NVP-LGK-974 WNT974 inhibitor

 

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