3-Bromopyruvic acid(Synonyms: 3-溴丙酮酸; Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP)

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3-Bromopyruvic acid (Synonyms: 3-溴丙酮酸; Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP) 纯度: 98.00%

3-Bromopyruvic acid 是己糖激酶 II (hexokinase II, HXK II) 抑制剂,是一种有效的针对肝癌细胞的抗肿瘤剂。

3-Bromopyruvic acid(Synonyms: 3-溴丙酮酸; Bromopyruvic acid;  Hexokinase II Inhibitor II, 3-BP)

3-Bromopyruvic acid Chemical Structure

CAS No. : 1113-59-3

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生物活性

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[1][2][3].

体外研究
(In Vitro)

3-Bromopyruvate enhances TRAIL-induced apoptosis in breast cancer cells[2].
3-Bromopyruvate (Bromopyruvic acid), a hexokinase II inhibitor, can induce apoptosis in hepatocellular carcinoma cells by inducing endoplasmic reticulum (ER) stress[2].
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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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
(In Vivo)

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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (BALB/c; 4-5-weeks old and 18-20 g)[2]
Dosage: 8 mg/kg
Administration: I.p.; every 4 days for 28 days
Result: Showed antitumor efficacy in tumor xenografts.

分子量

166.96

Formula

C3H3BrO3

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.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 250 mg/mL (1497.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.9895 mL 29.9473 mL 59.8946 mL
5 mM 1.1979 mL 5.9895 mL 11.9789 mL
10 mM 0.5989 mL 2.9947 mL 5.9895 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Gan L, et al. Synergistic Effect of 3-Bromopyruvate in Combination with Rapamycin Impacted Neuroblastoma Metabolism by Inhibiting Autophagy. Onco Targets Ther. 2020;13:11125-11137. Published 2020 Oct 29.

    [2]. Chen Y, et al. 3 Bromopyruvate sensitizes human breast cancer cells to TRAIL induced apoptosis via the phosphorylated AMPK mediated upregulation of DR5. Oncol Rep. 2018;40(5):2435-2444.

    [3]. Zhang Q, et al. Hexokinase II inhibitor, 3-BrPA induced autophagy by stimulating ROS formation in human breast cancer cells. Genes Cancer. 2014;5(3-4):100-112.

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