https://www.selleckchem.com/ 2-Methoxyjuglone, a member of the 1,4-naphthoquinone family, was first obtained through semi-synthesis based on 2-hydroxyjuglone as the precursor in 1966. It has been isolated and identified from different plant species of the Juglandaceae, Sterculiaceae, and Proteaceae families. 2-Methoxyjuglone has been demonstrated to possess a wide range of biological activities, including antitumor, antifungal, and antibacterial activities; in addition, it has been shown to poison fish and inhibit seed germination. These properties make 2-methoxyjuglone a promising bioactive compound for pharmaceutical and agricultural purposes. This review article provides an overview of the current research progress on 2-methoxyjuglone for the first time, with a primary focus on the plant sources, extraction, identification, synthesis, and biological activities associated with this compound for further development. While the upregulation of cytochrome P450 family 24 subfamily A member 1 (CYP24A1) gene expression has been reported in colon cancer, its role in tumorigenesis remains largely unknown. In this study, we aimed to investigate the involvement of CYP24A1 in Wnt pathway regulation via the nuclear factor kappa B (NF-κB) pathway. The human colon cancer cell lines HCT-116 and Caco-2 were subjected to stimulation with interleukin-6 (IL-6) as well as tumor necrosis factor alpha (TNF-α), with subsequent treatment using the NF-κB pathway-specific inhibitor ammonium pyrrolidinedithiocarbamate (PDTC). Furthermore, CYP24A1 expression was subjected to knockdown via the use of small interfering RNA (siRNA). Subsequently, NF-κB pathway activation was determined by an electrophoretic mobility shift assay, and the transcriptional activity of β-catenin was determined by a dual-luciferase reporter assay. A mouse ulcerative colitis (UC)-associated carcinogenesis model was established, wherein TNF-α and the NF-κB pathway were blocked by anti-TNF-α monoclonal antibody and NF-κB