Background:

3-Bromopyruvic acid is a hexokinase II inhibitor, is an effective antitumor agent on the hepatoma cells.Target: hexokinase II in vitro: 3-BrPA dissociates HK II from this complex, causing cell death, and thus, having an anti-tumor effect. In vitro treatment of cells with 3-BrPA significantly inhibited their growth, as evaluated by MTT assay and adenosine triphosphate-tumor chemosensitivity assay (ATP-TCA). [1] 3-Bromopyruvic acid (3-BP) is a glycolytic inhibitor and a promising anticancer compound, induces oxidative stress and depletes cells of glutathione (GSH). [2]in vivo: 3-BrPA treatment (50 mg/kg ip. daily, 6 days/week for three weeks) is effective in the animal model by attenuating tumor growth and causing tumor necrosis. Toxic signs were not observed. The acute toxicity study provided an LD50 of 191.7 mg/kg for 3-BrPA. [1]

参考文献:
[1]. Gong L, 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 Jun;14(5):771-6.
[2]. Sadowska-Bartosz I, et al. Anticancer agent 3-bromopyruvic acid forms a conjugate with glutathione. Pharmacol Rep. 2016 Apr;68(2):502-5.