WNT-974 LGK974

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Chemical Information

Product name：WNT-974 LGK974	Purity：98%min
CAS NO：1243244-14-5	Solubility：DMSO : ≥ 32 mg/mL (80.72 mM)
Molecular Formula：C₂₃H₂₀N₆O	Package：Package according to customer requirements
Molecular Weight：396.445	Storage：Store at -20℃

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Remarks

LGK974, aslo known as is a selective and orally bioavailable Porcupine (PORCN) inhibitor under development for the treatment of cancers that are driven by the Wnt pathway in a Wnt ligand-dependent manner. WNT974 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational acylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine, a membrane-bound O-acyltransferase (MBOAT), is required for the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion and activity. Wnt signaling is dysregulated in a variety of cancers.

PORCN Inhibitors Related Products:

ETC-159; Wnt-C59

References

[1]. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci U S A. 2013 Dec 10;110(50):20224-9.

[2]. Tammela T, et al. A Wnt-producing niche drives proliferative potential and progression in lung adenocarcinoma. Nature. 2017 May 18;545(7654):355-359.