3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.
体外研究
3-Bromopyruvate enhances TRAIL-induced apoptosis in breast cancer cells.
3-Bromopyruvate (Bromopyruvic acid), a hexokinase II inhibitor, can induce apoptosis in hepatocellular carcinoma cells by inducing endoplasmic reticulum (ER) stress.
3-Bromopyruvate inhibits ATP generation and upregulates the expression of DR5. 3-Bromopyruvate upregulates CHOP, GRP78 and the phosphorylation of AMPK and augments TRAIL-induced Bax and caspase-3 levels.
Cell Viability Assay
Cell Line:
MCF-7 and MDA-MB-231 cells
Concentration:
40, 80, 160 or 320 µM
Incubation Time:
24 hours
Result:
3-Bromopyruvate (80 and 160 µmol/l) and TRAIL (400 ng/ml) significantly inhibited cell viability.
体内研究
3-Bromopyruvate (8 mg/kg; i.p.; every 4 days for 28 days) shows a synergistic antitumor effect in MCF-7 cell xenografts in nude mice.
Animal Model:
Female nude mice (BALB/c; 4-5-weeks old and 18-20 g)
Dosage:
8 mg/kg
Administration:
I.p.; every 4 days for 28 days
Result:
Showed antitumor efficacy in tumor xenografts.
分子式
C3H3BrO3
分子量
166.96
CAS号
1113-59-3
中文名称
3-溴丙酮酸;溴丙酮酸;3-溴庚酸;3-溴代丙酮酸
运输条件
Room temperature in continental US; may vary elsewhere.