PCI-34051

目录号:S2012

仅限科研使用

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

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1815.22 现货
RMB 1377.26 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的PCI-34051发表文献39篇:

产品安全说明书

HDAC抑制剂选择性比较

相关HDAC产品

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
HDAC8 [1]
(Cell-free assay)
10 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Assay
Methods Test Index PMID
Immunofluorescence SMC3 / Ac-SMC3 27072133

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
  • 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:[1]
  • Cell lines: A549 细胞系, Ovcar-3 细胞系
  • Concentrations: 5 μM
  • Incubation Time: 24 小时
  • Method: 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。

溶解度(25°C)

体外

体内

从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40%PEG300+5% tween80+50% H2O

5 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 296.32
化学式

C17H16N2O3

CAS号 950762-95-5
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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

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,: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: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: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。

摩尔浓度计算器

质量 浓度 体积 分子量

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