PCI-34051

For research use only. Not for use in humans.

目录号:S2012

PCI-34051 Chemical Structure

CAS No. 950762-95-5

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1815.22 现货
RMB 1377.26 现货
RMB 9582.3 现货
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客户使用Selleck生产的PCI-34051发表文献37篇:

产品安全说明书

HDAC抑制剂选择性比较

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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Jurkat NXrCPGQ1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NITQd2c4OiCqcoO= MVXHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDKeZJs[XRiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG|c3H5MEBIUTVyPUGx{txO MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzFzNkG0O{c,OjNzMU[xOFc9N2F-
NB-1 MoTTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPRWZhZPzJiaILz MnPqS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmIuOSClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTB;MUVOwG0> NVqyOGNQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxNVYyPDdpPkKzNVE3OTR5PD;hQi=>
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Huh7 Mn;RRY51cX[rcnHsJIF{e2G7 M{\DSlMh\GG7cx?= MkjXRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFch[2WubIOgZYZ1\XJiMzDkZZl{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2xMljPxE1? MoizQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV2OUC3NFAoRjJ3NEmwO|AxRC:jPh?=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Immunofluorescence
SMC3 / Ac-SMC3 ; 

PubMed: 27072133     


A and B, representative immunofluorescence analysis of total- and ac-SMC3 in G1-S synchronized MCF7 cells treated with the indicated concentrations of PCI-34051 for 6 and 12 h, respectively. MCF7 cells grown in complete medium were synchronized to G1-S phase by double thymidine block and released in the presence of different concentrations of PCI-34051 for 6 or 12 h. Cells were stained for DNA (Hoechst-H33342, blue) and with antibodies detecting total-SMC3 (green) and ac-SMC3 (red). Cells were analyzed by Nikon C2 confocal microscope; images were taken at 20× magnification (z-series) using the NIS elements software, z-stacked, and processed using FIJI.

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 59 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble
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 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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