TEPP-46 is a potent and selective activator of pyruvate kinase M2 (PKM2), an enzyme involved in the regulation of glycolysis. Its primary application lies in cancer research, where it modulates the metabolic reprogramming characteristic of tumor cells. By activating PKM2, TEPP-46 shifts cellular metabolism from aerobic glycolysis (the Warburg effect) toward more oxidative phosphorylation, which can suppress tumor growth and proliferation. This compound is widely used as a pharmacological tool to study the role of PKM2 in cancer cell metabolism, offering insights into how metabolic pathways influence cell signaling, gene expression, and tumor progression. In preclinical studies, TEPP-46 has demonstrated the ability to reduce cancer cell growth in models of lung, breast, and colon cancers, making it a valuable probe for evaluating PKM2-targeted therapies. Additionally, TEPP-46 has been used to investigate metabolic dependencies in immune cells and has shown potential in enhancing anti-tumor immune responses by altering the metabolic environment of the tumor. Its application extends beyond oncology into studies of cellular metabolism, metabolic diseases, and mitochondrial function, supporting the development of metabolism-based therapeutic strategies.