NVP-LGK974 is a potent and selective inhibitor of porcupine (PORCN), an enzyme essential for the post-translational modification and secretion of Wnt proteins. By inhibiting PORCN, NVP-LGK974 effectively blocks Wnt signaling, a pathway frequently dysregulated in various cancers, particularly those with mutations leading to constitutive Wnt activation. This compound is primarily used in preclinical research to study Wnt-dependent tumor models, including colorectal, pancreatic, and other solid tumors. It has demonstrated antitumor activity in models where tumor growth is driven by autocrine or paracrine Wnt signaling. NVP-LGK974 is also employed to investigate the role of Wnt signaling in tissue regeneration, stem cell maintenance, and developmental biology. Due to its ability to suppress Wnt pathway activation, it serves as a valuable tool compound in oncology drug discovery, helping validate PORCN as a therapeutic target and guiding the development of new cancer therapies. Its use is largely confined to laboratory and experimental settings, supporting mechanistic studies and proof-of-concept experiments in vivo and in vitro.