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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)是PFKFB3的小分子抑制劑，對(duì)人源重組PFKFB3蛋白的IC50為22.9 μM，而且不抑制PFK-1活性。它能夠抑制葡萄糖吸收、減少胞內(nèi)Fru-2,6-BP, lactate, ATP, NAD+ 和 NADH的濃度。
3PO Chemical Structure
CAS: 18550-98-6
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
3PO相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | PFKFB3 PFKFB4 | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)產(chǎn)品 | PFK15 PFK158 KAN0438757 | 點(diǎn)擊展開(kāi) |
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) MAPK抑制劑庫(kù) DNA損傷/ DNA修復(fù)化合物庫(kù) 細(xì)胞周期化合物庫(kù) | 點(diǎn)擊展開(kāi) |
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | 3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one)是PFKFB3的小分子抑制劑，對(duì)人源重組PFKFB3蛋白的IC50為22.9 μM，而且不抑制PFK-1活性。它能夠抑制葡萄糖吸收、減少胞內(nèi)Fru-2,6-BP, lactate, ATP, NAD+ 和 NADH的濃度。 | ||
|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 3PO主要通過(guò)與Fru-6-P競(jìng)爭(zhēng)，抑制PFKFB3，而不抑制純化的PFK-1活性。在多種人源惡性血液腫瘤和癌細(xì)胞系中，3PO可顯著地減緩其細(xì)胞增殖(IC50=1.4-24 μM)。相較于正常的人類氣道上皮細(xì)胞，3PO選擇性對(duì)轉(zhuǎn)染了ras的氣道上皮細(xì)胞具有抑制生長(zhǎng)作用。3PO可引起細(xì)胞周期G2-M期阻滯[1]。 | |||
|---|---|---|---|---|
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | Jurkat細(xì)胞 | ||
| 濃度 | 10 μM | |||
| 孵育時(shí)間 | 0, 4, 8, 16, 24, 36 h | |||
| 方法 | 將Jurkat細(xì)胞以1 × 105/mL密度鋪于含10%胎牛血清和50 μg/mL gentamicin sulfate的RPMI 1640培養(yǎng)基中。用vehicle或10 μM 3PO處理細(xì)胞，處理時(shí)間為0, 4, 8, 16, 24 或 36 h。然后分析其細(xì)胞周期。 |
|||
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 向攜瘤小鼠腹腔注射0.07 mg的3PO，3PO的給藥顯著減少了其胞內(nèi)Fru-2,6-BP的濃度、葡萄糖吸收以及腫瘤的生長(zhǎng)。它可抑制乳腺癌、白血病和肺癌細(xì)胞的腫瘤生長(zhǎng)[1]。向C57Bl/6小鼠靜脈注射3PO，檢測(cè)其在體內(nèi)藥代動(dòng)力學(xué)參數(shù)：CL=2312 mL/min/kg, T1/2=0.3 hr, Cmax=113 ng/ml, AUC0-inf=36 ng/hr/ml。在白血病高度相關(guān)的小鼠模型中，3PO具有有效抗腫瘤活性[2]。 | |
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 攜瘤小鼠(BALB/c裸鼠或C57Bl/6小鼠) |
| Dosages | 0.07 mg/g | |
| Administration | i.p. | |
化學(xué)信息&溶解度
| 分子量 | 210.23 | 分子式 | C13H10N2O |
| CAS號(hào) | 18550-98-6 | SDF | Download 3PO SDF |
| Smiles | C1=CC(=CN=C1)C=CC(=O)C2=CC=NC=C2 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 42 mg/mL ( (199.78 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Ethanol : 11 mg/mL (52.32 mM) Water : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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