3PO

製品コードS7639 バッチS763902

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

10 mg/mL (47.56 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-ピリジニル)-1-(4-ピリジニル)-2-プロペン-1-オン)は、PFKFB3の低分子阻害剤で、組換えヒトPFKFB3タンパク質に対するIC50は22.9 μMであり、PFK-1活性は阻害しません。これはグルコースの取り込みを抑制し、Fru-2,6-BP、乳酸、ATP、NAD+、およびNADHの細胞内濃度を低下させます。
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.
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. 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.

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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