3PO

製品コードS7639 バッチS763903

印刷

化学情報

Chemical Structure Synonyms 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H10N2O
分子量 210.23 CAS No. 18550-98-6
Solubility (25°C)* 体外 DMSO 42 mg/mL (199.78 mM)
Ethanol 11 mg/mL (52.32 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
7.0mg/ml Taking the 1 mL working solution as an example, add 100 μL of 70 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 make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. 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 3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one) is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
in vitro 3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. 3PO can cause G2-M phase arrest[1].
in vivo i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo[1]. The PK properties of 3PO are examined in C57Bl/6 mice intravenously administered 3PO: clearance CL=2312 mL/min/kg, T1/2=0.3 hr, Cmax=113 ng/ml, AUC0-inf=36 ng/hr/ml. 3PO is reported to have potent activity against a highly relevant mouse model of leukemia[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Jurkat cells
濃度 10 μmol/L
反応時間 0, 4, 8, 16, 24, or 36 h
実験の流れ

Jurkat cells are plated at 1 × 105/mL in RPMI 1640 supplemented with 10% fetal bovine serum and 50 μg/mL gentamicin sulfate. Cells are immediately treated with vehicle or 10 μmol/L 3PO for 0, 4, 8, 16, 24, or 36 h. Cell cycle analysis is done.
動物実験 動物モデル tumor bearing mice (BALB/c nude mice or C57Bl/6 female mice background)
投薬量 0.07 mg/g
投与方法 i.p.

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：

Short isoform thymic stromal lymphopoietin reduces inflammation and aerobic glycolysis of asthmatic airway epithelium by antagonizing long isoform thymic stromal lymphopoietin [ Respir Res, 2022, 23(1):75] PubMed: 35351157
STAT3 signaling mediates peritoneal fibrosis by activating hyperglycolysis [ Am J Transl Res, 2022, 14(10):7552-7565] PubMed: 36398234
Hypoxic postconditioning promotes neurogenesis by modulating the metabolism of neural stem cells after cerebral ischemia [ Exp Neurol, 2021, 347:113871] PubMed: 34563509
The role of macrophage-fibroblast interaction in lipopolysaccharide-induced pulmonary fibrosis: an acceleration in lung fibroblast aerobic glycolysis [ Lab Invest, 2021, 10.1038/s41374-021-00701-7] PubMed: 34775492
HMGB1-activated fibroblasts promote breast cancer cells metastasis via RAGE/aerobic glycolysis [ Neoplasma, 2021, 68(1):71-78] PubMed: 33030958
PI3K-Akt-mTOR/PFKFB3 pathway mediated lung fibroblast aerobic glycolysis and collagen synthesis in lipopolysaccharide-induced pulmonary fibrosis [ Lab Invest, 2020, 100(6):801-811] PubMed: 32051533
PI3K-Akt-mTOR/PFKFB3 pathway mediated lung fibroblast aerobic glycolysis and collagen synthesis in lipopolysaccharide-induced pulmonary fibrosis. [ Lab Invest, 2020, 10.1038/s41374-020-0404-9] PubMed: 32051533
Targeting PFKFB3 sensitizes chronic myelogenous leukemia cells to tyrosine kinase inhibitor [ Oncogene, 2018, 37(21):2837-2849] PubMed: 29511345

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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