3PO

製品コードS7639 バッチS763901

印刷

化学情報

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

42 mg/mL (199.78 mM)

Water

Insoluble

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.

* <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. This compound 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. It 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 this compound are examined in C57Bl/6 mice intravenously administered this chemical: clearance CL=2312 mL/min/kg, T_1/2=0.3 hr, C_max=113 ng/ml, AUC_0-inf=36 ng/hr/ml. It 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.

参考

https://pubmed.ncbi.nlm.nih.gov/18202014/
https://pubmed.ncbi.nlm.nih.gov/23674815/

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：

KUS121, a novel VCP modulator, attenuates atherosclerosis development by reducing ER stress and inhibiting glycolysis through the maintenance of ATP levels in endothelial cells [ Atherosclerosis, 2025, 405:119223]	PubMed: 40339363
GLP-1R activation attenuates the progression of pulmonary fibrosis via disrupting NLRP3 inflammasome/PFKFB3-driven glycolysis interaction and histone lactylation [ J Transl Med, 2024, 22(1):954]	PubMed: 39434134
Evolutionary genomics identifies host-directed therapeutics to treat intracellular bacterial infections [ bioRxiv, 2023, 10.1101/2023.08.01.551011]	PubMed: None
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

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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