LGK-974
| CAS No. | 1243244-14-5 | Cat. No. | BCP08495 |
| Name | LGK-974 | ||
| Synonyms | LGK 974;LGK974; WNT974; WNT 974; WNT-974; | ||
| Formula | C23H20N6O | M. Wt | 396.44 |
| 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. | ||
| Pathways | Wnt/Stem Cell | ||
| Targets | Porcupine | ||
Structure
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