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3-Bromopyruvic acid

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Chemical Structure| 1113-59-3 同义名 : Bromopyruvic acid;Hexokinase II Inhibitor II, 3-BP;NSC 62343;NSC 11731;β-Bromopyruvic acid;3-BP;Hexokinase II Inhibitor II;3-Bromopyruvate
CAS号 : 1113-59-3
货号 : A376712
分子式 : C3H3BrO3
纯度 : 96%
分子量 : 166.958
MDL号 : MFCD00002587
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(628.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 250 mg/mL(1497.38 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 3-Bromopyruvate (3-BrPA) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-BrPA can induce growth inhibition in a dose-dependent pattern by cell apoptosis. 3-BrPA combined with rapamycin played a synergistic suppression role in NB cells, affected the cell apoptosis, cell cycle and the metabolic pathway[3]. Low concentration of 3-BrPA significantly affected both glutaminolysis and TCA cycle functions, through inhibition of isocitrate dehydrogenase, α-ketoglutarate dehydrogenase and succinate dehydrogenase. Additionally, 3-BrPA treatment significantly decreased the reduced status of thiol groups in HepG2 cells without proportional increase of oxidizing groups, suggesting that these chemical groups are the target of alkylation reactions induced by 3-BrPA[4]. 3-BrPA synergistically sensitized breast cancer cells to TRAIL‑induced apoptosis via the upregulation of death receptor 5 (DR5). And the protein levels of glucose‑related protein 78 (GRP78) and CCAAT‑enhancer‑binding protein homologous protein (CHOP) increased following treatment with 3-BrPA. 3-BrPA sensitized breast cancer cells to TRAIL via the AMPK (adenosine monophosphate-activated protein kinase)-mediated upregulation of DR5[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.99mL

1.20mL

0.60mL

29.95mL

5.99mL

2.99mL

59.90mL

11.98mL

5.99mL
参考文献

[1]Sadowska-Bartosz I, Szewczyk R, et al. Anticancer agent 3-bromopyruvic acid forms a conjugate with glutathione. Pharmacol Rep. 2016 Apr;68(2):502-5.

[2]Gong L, Wei Y, 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.

[3]Gan L, Ren Y, Lu J, Ma J, Shen X, Zhuang Z. Synergistic Effect of 3-Bromopyruvate in Combination with Rapamycin Impacted Neuroblastoma Metabolism by Inhibiting Autophagy. Onco Targets Ther. 2020 Oct 29;13:11125-11137

[4]Jardim-Messeder D, Moreira-Pacheco F. 3-Bromopyruvic Acid Inhibits Tricarboxylic Acid Cycle and Glutaminolysis in HepG2 Cells. Anticancer Res. 2016 May;36(5):2233-41

[5]Chen Y, Wei L, Zhang X, Liu X, Chen Y, Zhang S, Zhou L, Li Q, Pan Q, Zhao S, Liu H. 3‑Bromopyruvate sensitizes human breast cancer cells to TRAIL‑induced apoptosis via the phosphorylated AMPK‑mediated upregulation of DR5. Oncol Rep. 2018 Nov;40(5):2435-2444