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PCI-34051
PCI-34051是一種有效的，特異性的HDAC8抑制劑，無細胞試驗中IC50為10 nM。比作用于HDAC1和6選擇性高200多倍，比作用于HDAC2， 3，和10選擇性高1000倍。PCI-34051可誘導(dǎo)半胱天冬酶依賴的凋亡。
PCI-34051 Chemical Structure
CAS: 950762-95-5
產(chǎn)品質(zhì)控
批次：
純度：
99.79%
99.79
PCI-34051相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| BE(2)-C | Function assay | 6 uM | 72 hrs | Inhibition of HDAC8 in human BE(2)-C cells assessed as upregulation of p21/CDKN1 gene expression at 6 uM after 72 hrs by RT-PCR analysis relative to control | 29190092 |
| BE(2)-C | Function assay | 6 uM | 72 hrs | Inhibition of HDAC8 in human BE(2)-C cells assessed as upregulation of TrkA/NTRK1 gene expression at 6 uM after 72 hrs by RT-PCR analysis relative to control | 29190092 |
| BE(2)-C | Function assay | 6 uM | 72 hrs | Inhibition of HDAC8 in human BE(2)-C cells assessed as upregulation of TH gene expression at 6 uM after 72 hrs by RT-PCR analysis relative to control | 29190092 |
| BE(2)-C | Function assay | 6 uM | 6 days | Induction of outgrowth of neurofilament positive neutrite-like structures in human BE(2)-C cells at 6 uM after 6 days by DAPI-staining based microscopic analysis | 29190092 |
| MT2 | Growth inhibition assay | 72 hrs | Growth inhibition of human MT2 cells incubated for 72 hrs by MTS assay, GI50=15μM | 23116147 | |
| NB-1 | Growth inhibition assay | 72 hrs | Growth inhibition of human NB-1 cells incubated for 72 hrs by MTS assay, GI50=14μM | 23116147 | |
| Jurkat | Growth inhibition assay | 72 hrs | Growth inhibition of human Jurkat cells incubated for 72 hrs by MTS assay, GI50=11μM | 23116147 | |
| LAN1 | Growth inhibition assay | 72 hrs | Growth inhibition of human LAN1 cells incubated for 72 hrs by MTS assay, GI50=3.9μM | 23116147 | |
| MT4 | Growth inhibition assay | 72 hrs | Growth inhibition of human MT4 cells incubated for 72 hrs by MTS assay, GI50=25μM | 23116147 | |
| Huh7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50=1.8μM | 25490700 | |
| HuH7 | Cytotoxicity assay | 3 days | Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50=11μM | 25490700 | |
| Sf9 | Function assay | 5 mins | Inhibition of recombinant full-length human C-terminal FLAG-His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 35 mins by fluoresce, IC50=3.8μM | 28835796 | |
| Sf9 | Function assay | 5 mins | Inhibition of recombinant human full-length C-terminal His-tagged HDAC3 (395 to 489 residues)/human NCOR2 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate pretreated for 5 mins followed by substrate addition measured, IC50=7.1μM | 28835796 | |
| Sf9 | Function assay | 5 mins | Inhibition of recombinant human full-length C-terminal His-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-L-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 35 mins by fluorescence assay, IC50=31μM | 28835796 | |
| BE(2)-C | Cytotoxicity assay | 72 hrs | Cytotoxicity against human BE(2)-C cells assessed as reduction in cell viability by measuring metabolic activity after 72 hrs by WST-8 assay, IC50=19.9μM | 29190092 | |
| Sf9 | Function assay | 90 mins | Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC1 expressed in fall armyworm Sf9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorimetric analysis, IC50=28.3μM | 29190092 | |
| Sf9 | Function assay | 90 mins | Inhibition of recombinant human full length HDAC6 expressed in fall armyworm Sf9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorimetric analysis, IC50=48.2μM | 29190092 | |
| Jurkat | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay, IC50=4.5μM | 29533873 | |
| MOLT4 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50=9.4μM | 29533873 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEL cells after 48 hrs by MTT assay, IC50=10.8μM | 29533873 | |
| SK-N-BE(2) | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50=16.9μM | 29533873 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50=19.2μM | 29533873 | |
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by MTS assay, GI50=2.01μM | 30004697 | |
| K562R | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562R cells after 72 hrs by MTS assay, GI50=2.2μM | 30004697 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, GI50=2.64μM | 30004697 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay, GI50=2.66μM | 30004697 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, GI50=2.97μM | 30004697 | |
| Sf9 | Function assay | 40 mins | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected insect cells measured after 40 mins by HDAC-Glo1/2 luminescent assay, IC50=0.03162μM | 30964290 | |
| SK-N-BE(2)C | Anticlonogenic assay | 96 hrs | Anticlonogenic activity in human SK-N-BE(2)C cells assessed as reduction in cell proliferation incubated for 96 hrs by crystal violet staining based assay, GI50=15μM | 31630054 | |
| SH-SY5Y | Cytotoxicity assay | Cytotoxicity against human SH-SY5Y cells expressing TP53 by CellTiter96 AQueous one solution cell proliferation assay | 28835796 | ||
| IMR5 | Cytotoxicity assay | Cytotoxicity against human IMR5 cells expressing TP53 by CellTiter96 AQueous one solution cell proliferation assay | 28835796 | ||
| SK-N-AS | Cytotoxicity assay | Cytotoxicity against human SK-N-AS cells expressing TP53 mutation by CellTiter96 AQueous one solution cell proliferation assay | 28835796 | ||
| Kelly | Cytotoxicity assay | Cytotoxicity against human Kelly cells expressing TP53 mutation by CellTiter96 AQueous one solution cell proliferation assay | 28835796 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Jurkat | Antiproliferative assay | Antiproliferative activity against human Jurkat cells by alamar blue assay, GI50=2.4μM | 29505935 | ||
| HUT78 | Antiproliferative assay | Antiproliferative activity against human HUT78 cells by alamar blue assay, GI50=2.4μM | 29505935 | ||
| HSB2 | Antiproliferative assay | Antiproliferative activity against human HSB2 cells by alamar blue assay, GI50=2.4μM | 29505935 | ||
| MOLT4 | Antiproliferative assay | Antiproliferative activity against human MOLT4 cells by alamar blue assay, GI50=2.4μM | 29505935 | ||
| BL21 (DE3) | Function assay | Binding affinity to human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method, Kd=0.0751μM | 30347148 | ||
| BL21 (DE3) | Function assay | Inhibition of human His-thioredoxin-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=0.0777μM | 30347148 | ||
| BL21 (DE3) | Function assay | Binding affinity to Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells by ITC method, Kd=0.367μM | 30347148 | ||
| BL21 (DE3) | Function assay | Inhibition of Schistosoma mansoni His-tagged HDAC8 expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=0.4358μM | 30347148 | ||
| BL21 (DE3) | Function assay | Inhibition of human His-thioredoxin-tagged HDAC8 mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=1μM | 30347148 | ||
| BL21 (DE3) | Function assay | Inhibition of human His-thioredoxin-tagged HDAC8 mL6 mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=1.63μM | 30347148 | ||
| BL21 (DE3) | Function assay | Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6 mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=2.7μM | 30347148 | ||
| BL21 (DE3) | Function assay | Inhibition of human His-thioredoxin-tagged HDAC8 mL1/mL6/L179I mutant expressed in Escherichia coli BL21 (DE3) cells using Fluor de Lys (R)-HDAC8 as substrate by fluorometric method, IC50=5μM | 30347148 | ||
| Sf9 | Function assay | Inhibition of C-terminal FLAG/His-tagged full length human HDAC1 expressed in baculovirus infected Sf9 insect cells using Z(Ac)Lys-AMC as substrate by fluorometric method, IC50=28.3μM | 30347148 | ||
| Sf9 | Function assay | Inhibition of N-terminal GST-tagged full length human HDAC6 expressed in baculovirus infected Sf9 insect cells using Z(Ac)Lys-AMC as substrate by fluorometric method, IC50=48.2μM | 30347148 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | PCI-34051是一種有效的，特異性的HDAC8抑制劑，無細胞試驗中IC50為10 nM。比作用于HDAC1和6選擇性高200多倍，比作用于HDAC2， 3，和10選擇性高1000倍。PCI-34051可誘導(dǎo)半胱天冬酶依賴的凋亡。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | PCI-34051有效作用于HDAC8，Ki為10 nM。與其他I型HDACs包括HDAC1相比，PCI-34051更高選擇性作用于HDAC8。比作用于HDAC1和HDAC6選擇性高200倍，比作用于 HDAC2, HDAC3 和HDAC10選擇性高1000倍。PCI-34051抑制卵巢瘤細胞系OVCAR-3，GI50為6 μM，細胞死亡率為15%。PCI-34051濃度低于25 μM 時，處理敏感細胞系，在24小時而非更早時間點，觀察不到顯著的微管蛋白，也觀察不到組蛋白乙酰化。PCI-34051 作用于T細胞惡性腫瘤衍生的細胞系，誘導(dǎo)選擇性的細胞毒性作用。PCI-34051 誘導(dǎo)caspase依賴性凋亡。使用5 μM PCI-34051處理后，在不同時間點測量caspase-3活性, 在12 到24 到48 小時觀察到活性水平提高，凋亡的另一種標志, 與更高水平caspase 活性一致。PCI-34051不刺激 Bid 分裂, Bid 分裂是外在凋亡通路的特性影響。P116 和 J.RT3-T.5 對PCI-34051敏感，PLCγ1缺陷的J.gamma1系顯著降低 PCI-34051誘導(dǎo)凋亡的程度。此外, 穩(wěn)定的鈣水平也強烈影響PCI-34051誘導(dǎo)的凋亡。PCI-34051誘導(dǎo)細胞色素 c從線粒體中釋放。[1] |
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|---|---|---|---|---|
| 激酶實驗 | 組蛋白去乙酰化酶活性 | |||
| 使用96孔實驗板上，反應(yīng)體積為100 μL，在熒光酶標儀上測量PCI-34051特性。HDAC 蛋白在反應(yīng)buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% DMSO, pH7.4,伴有牛血清蛋白，濃度為0-0.05%)中與不同濃度PCI-34051混合，再溫育15分鐘，測定每種酶。加入胰蛋白酶，終濃度為50 nM,加入乙酰基-gly-Ala-(N-乙?；?Lys)-氨基-4-甲基香豆素，終濃度為25-100 μM，開始反應(yīng)。停滯30分鐘后, 使用激發(fā)波長為335 nm，檢測波長為460 nm，在30分鐘時間范圍測量熒光值。測量的熒光值的增量用了衡量反應(yīng)速率 。 | ||||
| 細胞實驗 | 細胞系 | A549 細胞系, Ovcar-3 細胞系 | ||
| 濃度 | 5 μM | |||
| 孵育時間 | 24 小時 | |||
| 方法 | 腫瘤細胞系和人臍靜脈內(nèi)皮細胞培養(yǎng)至少兩次倍增時間，PCI-34051處理末期，通過Alamar Blue熒光細胞增殖檢測實驗監(jiān)測生長。PCI-34051重復(fù)三份加入96孔板中。使用四參數(shù)方程，通過非線性回歸估量抑制 50% 細胞生長所需濃度(GI50)和95%置信區(qū)間。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Immunofluorescence | SMC3 / Ac-SMC3 |
|
27072133 | |
化學(xué)信息&溶解度
| 分子量 | 296.32 | 分子式 | C17H16N2O3 |
| CAS號 | 950762-95-5 | SDF | Download PCI-34051 SDF |
| Smiles | COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 59 mg/mL ( (199.1 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(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：如該濃度超過該批次藥物DMSO溶解度，請先聯(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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