3-Bromopyruvic acid (3-BP) is a hexokinase II inhibitor with Ki of 2.4 mM, is an effective antitumor agent on the hepatoma cells[1].
3-BP decreases proliferation of hepatocellular carcinoma BEL-7402 cells that express hexokinase II, an isoform of hexokinase overexpressed in many cancers[2,3].
3-BP reduces tumor growth and induces tumor necrosis in a hepatocellular carcinoma mouse xenograft model when administered at a dose of 50 mg/kg per day, six days per week, for three weeks[2].
References:
[1]. Ihrlund L S, Hernlund E, Khan O, et al. 3-Bromopyruvate as inhibitor of tumour cell energy metabolism and chemopotentiator of platinum drugs. Molecular Oncology, 2008, 2(1): 94-101.
[2]. Gong L, Wei Y, Yu X, et al. 3-Bromopyruvic acid, a hexokinase II inhibitor, is an effective antitumor agent on the hepatoma cells: In vitro and in vivo findings. Anticancer Agents Med. Chem, 2014, 14(5): 771-776.
[3]. Lis P, Dylag M, Niedźwiecka K, et al. The HK2 dependent "Warburg Effect" and mitochondrial oxidative phosphorylation in cancer: Targets for effective therapy with 3-bromopyruvate. Molecules, 2016, 21(12): E1730.
