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3-Bromopyruvate (3-BP) is a small molecule alkylating agent and a potent inhibitor of glycolysis. It acts primarily by inhibiting hexokinase-2 (HK2) and glyceraldehyde-3-phosphate dehydrogenase (GAPDH), thereby disrupting the Warburg effect in cancer cells. By blocking glycolytic flux and the pentose phosphate pathway (PPP), it depletes cellular ATP and nucleotide precursors, which sensitizes tumors to other treatments such as radiation or chemotherapy. 3-BP has been investigated for various cancers with high glycolytic rates, including pancreatic cancer and hepatocellular carcinoma, and is often studied as a metabolic sensitizer in combination therapies.
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