LGK974 (1243244-14-5) Description
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.
LGK974 (1243244-14-5) Specifications
|Synonym||LGK974; LGK-974; LGK 974; WNT974; WNT 974; WNT-974.|
|Solubility||Soluble in DMSO|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||> >5 years if stored properly|
|Application||In preparation of a product treating polycystic kidney disease is disclosed|