3PO
别名: 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one)是PFKFB3的小分子抑制剂，对人源重组PFKFB3蛋白的IC50为22.9 μM，而且不抑制PFK-1活性。它能够抑制葡萄糖吸收、减少胞内Fru-2,6-BP, lactate, ATP, NAD+ 和 NADH的浓度。
3PO Chemical Structure
CAS: 18550-98-6
产品质控
批次：
纯度：
99.94%
99.94
3PO相关产品
| 相关靶点 | PFKFB3 PFKFB4 | 点击展开 |
|---|---|---|
| 相关产品 | PFK15 PFK158 KAN0438757 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | 3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one)是PFKFB3的小分子抑制剂，对人源重组PFKFB3蛋白的IC50为22.9 μM，而且不抑制PFK-1活性。它能够抑制葡萄糖吸收、减少胞内Fru-2,6-BP, lactate, ATP, NAD+ 和 NADH的浓度。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 3PO主要通过与Fru-6-P竞争，抑制PFKFB3，而不抑制纯化的PFK-1活性。在多种人源恶性血液肿瘤和癌细胞系中，3PO可显著地减缓其细胞增殖(IC50=1.4-24 μM)。相较于正常的人类气道上皮细胞，3PO选择性对转染了ras的气道上皮细胞具有抑制生长作用。3PO可引起细胞周期G2-M期阻滞[1]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | Jurkat细胞 | ||
| 浓度 | 10 μM | |||
| 孵育时间 | 0, 4, 8, 16, 24, 36 h | |||
| 方法 | 将Jurkat细胞以1 × 105/mL密度铺于含10%胎牛血清和50 μg/mL gentamicin sulfate的RPMI 1640培养基中。用vehicle或10 μM 3PO处理细胞，处理时间为0, 4, 8, 16, 24 或 36 h。然后分析其细胞周期。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | 向携瘤小鼠腹腔注射0.07 mg的3PO，3PO的给药显著减少了其胞内Fru-2,6-BP的浓度、葡萄糖吸收以及肿瘤的生长。它可抑制乳腺癌、白血病和肺癌细胞的肿瘤生长[1]。向C57Bl/6小鼠静脉注射3PO，检测其在体内药代动力学参数：CL=2312 mL/min/kg, T1/2=0.3 hr, Cmax=113 ng/ml, AUC0-inf=36 ng/hr/ml。在白血病高度相关的小鼠模型中，3PO具有有效抗肿瘤活性[2]。 | |
|---|---|---|
| 动物实验 | Animal Models | 携瘤小鼠(BALB/c裸鼠或C57Bl/6小鼠) |
| Dosages | 0.07 mg/g | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 210.23 | 分子式 | C13H10N2O |
| CAS号 | 18550-98-6 | SDF | Download 3PO SDF |
| Smiles | C1=CC(=CN=C1)C=CC(=O)C2=CC=NC=C2 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 42 mg/mL ( (199.78 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 11 mg/mL (52.32 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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