Protein Inhibitors - LGK 974 (CAS: 1243244-14-5)

LGK 974 (CAS: 1243244-14-5)

Catalog #：EBC51135

Biological Activity

Synonyms

NVP-LGK974, WNT974

Chemical Name

2-[5-methyl-6-(2-methylpyridin-4-yl)pyridin-3-yl]-N-(5-pyrazin-2-ylpyridin-2-yl)acetamide

Application

LGK 974 is a potent and specific small molecule Porcupine (PORCN) inhibitor

CAS Number

1243244-14-5

Purity

≥98.0%

Molecular Weight

396.44

Molecular Formula

C₂₃H₂₀N₆O

SMILES

CC1=C(N=CC(=C1)CC(=O)NC2=NC=C(C=C2)C3=NC=CN=C3)C4=CC(=NC=C4)C

Target & IC50

PORCN

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	2.5224 ml	12.6122 ml	25.2244 ml
5 mM	0.5045 ml	2.5224 ml	5.0449 ml
10 mM	0.2522 ml	1.2612 ml	2.5224 ml
50 mM	0.0504 ml	0.2522 ml	0.5045 ml

Solubility
DMSO: 19.8 mg/mL (49.9 mM)

Product Description

LGK 974 is a potent and specific small molecule Porcupine (PORCN) inhibitor. Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. LGK 974 greatly reduces Wnt secretion without decreasing its synthesis and without increasing cytotoxicity. LGK 974 is orally bioavailable in mice and induces tumor regression in mouse breast tumors produced by mammary tumor virus-driven Wnt1 signaling. Interestingly, it can also block carcinogenesis in other Wnt-related tumors at doses that have limited impact on stem cell renewal.