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WNT-974

Chemical Structure : WNT-974

CAS No.: 1243244-14-5

WNT-974 (LGK-974;LGK974;LGK 974;WNT 974;WNT974 )

Catalog No.: PC-45342Not For Human Use, Lab Use Only.

WNT-974 (LGK974) is a potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1 nM in the PORCN radioligand binding assay.

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Biological Activity

WNT-974 (LGK974) is a potent and specific small-molecule Porcupine (PORCN) inhibitor with IC50 of 1 nM in the PORCN radioligand binding assay.
WNT-974 potently inhibits Wnt signaling with IC50 of 0.4 nM, with no major cytotoxicity.
WNT-974 reduces Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2.
WNT-974 is potent and efficacious in multiple tumor models at well-tolerated doses in vivo.

Physicochemical Properties

M.Wt 396.4445
Formula C23H20N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

[2,4'-Bipyridine]-5-acetamide, 2',3-dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-

References

1. Liu J, et al. Proc Natl Acad Sci U S A. 2013 Dec 10;110(50):20224-9.

2. Jiang X, et al. Proc Natl Acad Sci U S A. 2013 Jul 30;110(31):12649-54.

3. Moon J, et al. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1649-1654.

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