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LGK974

Catalog No. T2618 CAS 1243244-14-5

Synonyms: NVP-LGK974, LGK-974, LGK 974, WNT974

LGK-974 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.

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LGK974, CAS 1243244-14-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LGK-974 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	NVP-LGK974, LGK-974, LGK 974, WNT974
Molecular Weight	396.454
Formula	C23H20N6O
CAS No.	1243244-14-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 73 mg/mL (184.1 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Obesity Compound Library Inhibitor Library Wnt/Hedgehog/Notch Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Stem Cell Differentiation Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

IWP-O1 Porcn-IN-1 ETC-159 IWP-2 IWP L6 LGK974 Wnt-C59 GNF-6231

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LGK974 1243244-14-5 干细胞 Porcupine WNT-974 LGK 974 WNT 974 WNT974 LGK-974 Inhibitor NVP-LGK974 inhibit inhibitor

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