t-5224

Description: T-5224 is a novel and selective inhibitor of c-Fos/activator protein-1 (AP-1) which is a transcriptional factor that regulates the expression of various genes associated with tumor invasion and migration. T-5224 has potential use in cancer and rheumatoid arthritis therapy. T-5224 ameliorates liver injury and improves survival through decreasing production of proinflammatory cytokines and chemokines in endotoxemic mice. T-5224 has been investigated in phase II human clinical trials. T-5224 (0-80 uM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner. T-5224 inhibited the invasion and migration of HNSCC cells in vitro, and prevented lymph node metastasis in head and neck cancer in an animal model.

References: Cancer Sci. 2016 May; 107(5):666-73; Drug Metab Dispos. 2011 May; 39(5):803-13.