Bromopyruvic acid (3-BP)

製品コードS5426 バッチS542602

印刷

化学情報

 Chemical Structure Synonyms 3-Bromopyruvic acid, 3-Bromopyruvate, Hexokinase II Inhibitor II Storage
(From the date of receipt)
3 years -20°C powder
化学式

C3H3BrO3

分子量 166.96 CAS No. 1113-59-3
Solubility (25°C)* 体外 DMSO 33 mg/mL (197.65 mM)
Water 33 mg/mL (197.65 mM)
Ethanol 33 mg/mL (197.65 mM)
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.650mg/ml (9.88mM) Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.650mg/ml (9.88mM) Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Bromopyruvic acid (3-BP) is a hexokinase II inhibitor with Ki of 2.4 mM for glycolysis/hexokinase inhibition. It is inhibitor of tumour cell energy metabolism and chemopotentiator of platinum drugs.
in vitro

Bromopyruvic acid, a glycolysis inhibitor, maintains haploidy to a certain extent in both OdG and EG1 haESCs, with no effect on the proliferation or pluripotency of the haESCs.[2]

in vivo

Bromopyruvic acid reduces the growth of RKO cells with CD36 knockdown at a significantly slower rate in xenograft model.[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mouse haESC lines AGH-OG-3 and AGH-EG-1
濃度 12.5 μg/mL
反応時間 12 days
実験の流れ

Mouse haESC lines AGH-OG-3 and AGH-EG-1 were cultured in M2iL mediums, which containing knockout DMEM, 15% fetal bovine serum, 1% GlutaMAX, 1% nonessential amino acids, 100 μM β-mercaptoethanol, 100 U Leukemia inhibitory factor, 3 μM CHIR99021, and 1 μM PD0325901. The cells are cultured at 37 ℃ with 5% CO2 in a humidified environment. 1,25-(OH)2D3 and 3-BrPA are used at a final concentration of 12.5 μg/mL and 5μM, respectively.

動物実験 動物モデル 4-week-old nude mice injected with RKO cells
投薬量 5 mg/kg/day
投与方法 i.p.

参考

  • https://www.sciencedirect.com/science/article/pii/S1574789108000045
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7815943/
  • https://pubmed.ncbi.nlm.nih.gov/31484922/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Photobiomodulation modulates mitochondrial energy metabolism and ameliorates neurological damage in an APP/PS1 mousmodel of Alzheimer's disease [ Alzheimers Res Ther, 2025, 17(1):72] PubMed: 40188044
GL-V9 inhibits the activation of AR-AKT-HK2 signaling networks and induces prostate cancer cell apoptosis through mitochondria-mediated mechanism [ iScience, 2024, 27(3):109246] PubMed: 38439974
Hexokinase 2 nonmetabolic function-mediated phosphorylation of IκBα enhances pancreatic ductal adenocarcinoma progression [ Cancer Sci, 2024, 10.1111/cas.16204] PubMed: 38801832
METTL14 modulates glycolysis to inhibit colorectal tumorigenesis in p53-wild-type cells [ EMBO Rep, 2023, e56325.] PubMed: 36794620
3-Bromopyruvate overcomes cetuximab resistance in human colorectal cancer cells by inducing autophagy-dependent ferroptosis [ Cancer Gene Ther, 2023, 10.1038/s41417-023-00648-5] PubMed: 37558749
ASPP2 suppresses tumour growth and stemness characteristics in HCC by inhibiting Warburg effect via WNT/β-catenin/HK2 axis [ J Cell Mol Med, 2023, 27(5):659-671] PubMed: 36752127
Microglial hexokinase 2 deficiency increases ATP generation through lipid metabolism leading to β-amyloid clearance [ Nat Metab, 2022, 4(10):1287-1305] PubMed: 36203054
Integration of glucose and cardiolipin anabolism confers radiation resistance of HCC [ Hepatology, 2022, 75(6):1386-1401] PubMed: 34580888
Inhibition of abnormally activated HIF-1α-GLUT1/3-glycolysis pathway enhances the sensitivity of hepatocellular carcinoma to 5-caffeoylquinic acid and its derivatives [ Eur J Pharmacol, 2022, S0014-2999(22)00105-4] PubMed: 35189090
Viral growth factor- and STAT3 signaling-dependent elevation of the TCA cycle intermediate levels during vaccinia virus infection [ PLoS Pathog, 2021, 17(2):e1009303] PubMed: 33529218

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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