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3PO

別名：3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one

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.

3PO化学構造

CAS No. 18550-98-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 44500 国内在庫あり
JPY 88500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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3PO関連製品

PFKFB阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
Jurkat Cell proliferation assay 10 uM 36 hrs Inhibition of cell proliferation of human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM incubated for 36 hrs by trypan blue dye exclusion assay ChEMBL
Jurkat Function assay 10 uM 4 hrs Reduction in Fru-2,6-BP production in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM measured within 4 hrs ChEMBL
Jurkat Function assay 10 uM 8 hrs Reduction in lactate secretion in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 8 hrs by lactate oxidase based colorimetric assay ChEMBL
Jurkat Function assay 10 uM 16 hrs Reduction in NADH level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 16 hrs ChEMBL
Jurkat Function assay 10 uM 24 hrs Reduction in NAD+ level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 24 hrs ChEMBL
Jurkat Function assay 10 uM 24 hrs Reduction in ATP level in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 24 hrs ChEMBL
Jurkat Function assay 10 uM 36 hrs Suppression of glycolytic flux into lactate in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM after 36 hrs by NMR spectroscopy ChEMBL
NHBE Growth inhibition assay 1 uM 48 to 72 hrs Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein at 1 uM incubated for 48 to 72 hrs by trypan blue dye exclusion assay ChEMBL
NHBE Growth inhibition assay 10 uM 48 to 72 hrs Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein at 10 uM incubated for 48 to 72 hrs by trypan blue dye exclusion assay ChEMBL
Jurkat Function assay 10 uM Reduction in 2-deoxy-glucose uptake in human Jurkat cells expressing inducible FLAG-tagged PFKFB at 10 uM measured within 4 hrs using [14C]-2-deoxy-glucose by scintillation counting method ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells expressing inducible FLAG-tagged PFKFB incubated for 48 hrs by trypan blue dye exclusion assay, IC50=1.4μM ChEMBL
NHBE Growth inhibition assay 48 to 72 hrs Growth inhibition of human NHBE cells immortalized with human telomerase and large-T antigen and transformed with mutated Ras protein incubated for 48 to 72 hrs by trypan blue dye exclusion assay, IC50=1.5μM ChEMBL
K562 Growth inhibition assay 48 hrs Growth inhibition of human K562 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=3.2μM ChEMBL
HL60 Growth inhibition assay 48 hrs Growth inhibition of human HL60 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=4.5μM ChEMBL
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=4.7μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells expressing un-altered PFKFB expression incubated for 48 hrs by trypan blue dye exclusion assay, IC50=8.9μM ChEMBL
CRL11174 Growth inhibition assay 48 hrs Growth inhibition of human CRL11174 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=15μM ChEMBL
LLC Growth inhibition assay 48 hrs Growth inhibition of mouse LLC cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=19μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells expressing inducible FLAG-tagged PFKFB in presence of doxycycline incubated for 48 hrs by trypan blue dye exclusion assay, IC50=19.3μM ChEMBL
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=24μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of PFKFB3+/-ht/LT/Ras human Jurkat cells and incubated for 48 hrs by trypan blue dye exclusion assay, IC50=26μM ChEMBL
A549 Growth inhibition assay 48 hrs Growth inhibition of human A549 cells incubated for 48 hrs by trypan blue dye exclusion assay, IC50=48μM ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of PFKFB3+/+ht/LT/Ras human Jurkat cells and incubated for 48 hrs by trypan blue dye exclusion assay, IC50=49μM ChEMBL
Jurkat Cell cycle assay Inhibition of cell cycle arrest in human Jurkat cells expressing inducible FLAG-tagged PFKFB assessed as accumulation at G2/M phase by propidium iodide staining based flow cytometry ChEMBL
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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.
Targets
PFKFB3 [2]
22.9 μM
In Vitro
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].
細胞実験 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.
In Vivo
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].
動物実験 動物モデル tumor bearing mice (BALB/c nude mice or C57Bl/6 female mice background)
投与量 0.07 mg/g
投与経路 i.p.

化学情報

分子量 210.23 化学式

C13H10N2O
CAS No. 18550-98-6 SDF Download 3PO SDFをダウンロードする
Smiles C1=CC(=CN=C1)C=CC(=O)C2=CC=NC=C2
保管

In vitro
Batch:

DMSO : 42 mg/mL ( (199.78 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 11 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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