PCI-34051
PCI-34051是一种有效的，特异性的HDAC8抑制剂，无细胞试验中IC50为10 nM。比作用于HDAC1和6选择性高200多倍，比作用于HDAC2， 3，和10选择性高1000倍。PCI-34051可诱导半胱天冬酶依赖的凋亡。
PCI-34051 Chemical Structure
CAS: 950762-95-5
产品质控
批次：
纯度：
99.79%
99.79
PCI-34051相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PCI-34051是一种有效的，特异性的HDAC8抑制剂，无细胞试验中IC50为10 nM。比作用于HDAC1和6选择性高200多倍，比作用于HDAC2， 3，和10选择性高1000倍。PCI-34051可诱导半胱天冬酶依赖的凋亡。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | PCI-34051有效作用于HDAC8，Ki为10 nM。与其他I型HDACs包括HDAC1相比，PCI-34051更高选择性作用于HDAC8。比作用于HDAC1和HDAC6选择性高200倍，比作用于 HDAC2, HDAC3 和HDAC10选择性高1000倍。PCI-34051抑制卵巢瘤细胞系OVCAR-3，GI50为6 μM，细胞死亡率为15%。PCI-34051浓度低于25 μM 时，处理敏感细胞系，在24小时而非更早时间点，观察不到显著的微管蛋白，也观察不到组蛋白乙酰化。PCI-34051 作用于T细胞恶性肿瘤衍生的细胞系，诱导选择性的细胞毒性作用。PCI-34051 诱导caspase依赖性凋亡。使用5 μM PCI-34051处理后，在不同时间点测量caspase-3活性, 在12 到24 到48 小时观察到活性水平提高，凋亡的另一种标志, 与更高水平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响。P116 和 J.RT3-T.5 对PCI-34051敏感，PLCγ1缺陷的J.gamma1系显著降低 PCI-34051诱导凋亡的程度。此外, 稳定的钙水平也强烈影响PCI-34051诱导的凋亡。PCI-34051诱导细胞色素 c从线粒体中释放。[1] |
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| 激酶实验 | 组蛋白去乙酰化酶活性 | |||
| 使用96孔实验板上，反应体积为100 μL，在荧光酶标仪上测量PCI-34051特性。HDAC 蛋白在反应buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% DMSO, pH7.4,伴有牛血清蛋白，浓度为0-0.05%)中与不同浓度PCI-34051混合，再温育15分钟，测定每种酶。加入胰蛋白酶，终浓度为50 nM,加入乙酰基-gly-Ala-(N-乙酰基-Lys)-氨基-4-甲基香豆素，终浓度为25-100 μM，开始反应。停滞30分钟后, 使用激发波长为335 nm，检测波长为460 nm，在30分钟时间范围测量荧光值。测量的荧光值的增量用了衡量反应速率 。 | ||||
| 细胞实验 | 细胞系 | A549 细胞系, Ovcar-3 细胞系 | ||
| 浓度 | 5 μM | |||
| 孵育时间 | 24 小时 | |||
| 方法 | 肿瘤细胞系和人脐静脉内皮细胞培养至少两次倍增时间，PCI-34051处理末期，通过Alamar Blue荧光细胞增殖检测实验监测生长。PCI-34051重复三份加入96孔板中。使用四参数方程，通过非线性回归估量抑制 50% 细胞生长所需浓度(GI50)和95%置信区间。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Immunofluorescence | SMC3 / Ac-SMC3 |
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27072133 | |
化学信息&溶解度
| 分子量 | 296.32 | 分子式 | C17H16N2O3 |
| CAS号 | 950762-95-5 | SDF | Download PCI-34051 SDF |
| Smiles | COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 59 mg/mL ( (199.1 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 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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