LGK974, Porcupine (Wnt) Inhibitor

Catalog No. size PriceQuantity
M60106-2D 10 mM DMSO (0.504 mL) $139
M60106-2S 2mg solid $139
M60106-10S 10mg solid $563


Product Information
Molecular Weight: 396.44
Formula: C23H20N6O
Purity: ≥98%
CAS#: 1243244-14-5
Solubility: DMSO up to 100 mM
Chemical Name: 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.


Biological Activity:

LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 ~0.4 nM. LGK974 potently inhibits Wnt signaling in vitro and in vivo, including reduction of the Wnt-dependent LRP6 phosphorylation and the expression of Wnt target genes, such as AXIN2. LGK974 is potent and efficacious in multiple tumor models at well-tolerated doses in vivo, including murine and rat mechanistic breast cancer models driven by MMTV–Wnt1 and a human head and neck squamouscell carcinoma model (HN30). We also show that head and neck cancer cell lines with loss-of-function mutations in the Notch signaling pathway have a high response rate to LGK974. Currently LGK974 is in the Phase I study to treat cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner.


How to Use:


  • In vitro:  LGK974 was suggested to be used at 0.1 µM final concentration in vitro to completely block Wnt protein secretion.
  • In vivo:  LGK974 was used to dose mice orally at 0.1-10 mg/kg once or twice per day to achieve good efficacy in xenograft models.  




  • 1. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. (2013) Proc Natl Acad Sci USA. 110(50):20224-9.
  • 2. Jiang X, et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. (2013) Proc Natl Acad Sci USA. 110(31):12649-54. 
  • 3. Shifeng Pan. Discovery of LGK974: A selective Porcupine inhibitor targeting Wnt signaling in cancer.  AACR Annual Meeting 2013.

Products are for research use only. Not for human use.

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