2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. PCI-34051

PCI-34051 是一种有效的选择性的 HDAC8 抑制剂，IC50 为 10 nM。

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PCI-34051 Chemical Structure

PCI-34051 Chemical Structure

CAS No. : 950762-95-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥679
In-stock
5 mg ￥617
In-stock
10 mg ￥1090
In-stock
50 mg ￥4275
In-stock
100 mg ￥7450
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

PCI-34051 相关抗体

Top Publications Citing Use of Products

    PCI-34051 purchased from MCE. Usage Cited in: Nucleic Acids Res. 2020 Apr 6;48(6):2912-2923.  [Abstract]

    Immunoblotting analysis of SIRT7 level in cells incubated with the HDAC8 inhibitor PCI-34051 (PCI), in the presence or absence of TGF-1 (5 ng/ml).

    查看 HDAC 亚型特异性产品:

    查看所有亚型
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

    IC50 & Target[1]

    HDAC8

    10 nM (IC50)

    HDAC6

    2.9 μM (IC50)

    HDAC1

    4 μM (IC50)

    HDAC10

    13 μM (IC50)

    体外研究
    (In Vitro)

    PCI-34051 inhibits pure recombinant HDAC8 with Ki of 10 nM with >200-fold selectivity over the other HDACs tested, including HDACs 1, 2, 3, 6 and 10. PCI-34051 is derived from a low molecular weight hydroxamic acid scaffold that possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs. PCI-34051 is found to induce apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, whereas doses as high as 20 μM has no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    PCI-34051 相关抗体:
    体内研究
    (In Vivo)

    Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    296.32

    Formula

    C17H16N2O3
    CAS 号
    性状

    固体

    颜色

    White to gray

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 30 mg/mL (101.24 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.3747 mL 16.8736 mL 33.7473 mL
    5 mM 0.6749 mL 3.3747 mL 6.7495 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (8.44 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.44 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.69%

    COA (171 KB) LCMS (100 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    Histone deacetylase activity is measured using a continuous trypsin-coupled assay. For inhibitor characterization, measurements are performed in a reaction volume of 100 μL-1 using 96-well assay plates in a fluorescence plate reader. For each isozyme, the HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% DMSO, pH 7.4, supplemented with bovine serum albumin at concentrations of 0-0.05% ) is mixed with inhibitor at various concentrations and allowed to incubate for 15 min. Trypsin is added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-amino-4-methylcoumarin is added to a final concentration of 25-100 μM to initiate the reaction. After a 30 min lag time, the fluorescence is measured over a 30 min time frame using an excitation wavelength of 355 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. Inhibition constants Ki(app) are obtained using the program BatchKi[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times, and growth is monitored at the end of compound exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer. Compounds (e.g.,PCI-34051) are assayed in triplicate wells in 96-well plates. The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from nonlinear regression using a four-parameter logistic equation[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    A mouse model of asthma is utilized. Briefly, healthy female BALB/C mice (n=72) aged 6-8 weeks and weighing 18-22 g are used. Animals are housed independently in a pathogen-free room and provided ad libitum access to water and standard food. Animals are housed for 1 week prior to experiment onset. Mice are divided into six treatment groups: normal control, simple asthma, Dexamethasone, Tubastatin A HCl, PCI-34051, and Givinostat. Sensitization is carried out for mice in the last five groups on the 1st, 8th and 15th day using ovalbumin (OVA, 20 μg) and aluminum hydroxide gel (2 mg). 7 days after the last sensitization, OVA (20 mg/mL) atomization is performed using an ultrasonic atomizing device (3 mL/min for 30 min, 3 times/week for 8 weeks). Dexamethasone (2.0 mg/kg), TSA (0.5 mg/kg), PCI-34051 (0.5 mg/kg) and Givinostat (0.5 mg/kg) are administered via intraperitoneal injection 30 min before excitation. In the normal control group, normal saline is used instead of OVA.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    PCI-34051 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3747 mL 16.8736 mL 33.7473 mL 84.3682 mL
    5 mM 0.6749 mL 3.3747 mL 6.7495 mL 16.8736 mL
    10 mM 0.3375 mL 1.6874 mL 3.3747 mL 8.4368 mL
    15 mM 0.2250 mL 1.1249 mL 2.2498 mL 5.6245 mL
    20 mM 0.1687 mL 0.8437 mL 1.6874 mL 4.2184 mL
    25 mM 0.1350 mL 0.6749 mL 1.3499 mL 3.3747 mL
    30 mM 0.1125 mL 0.5625 mL 1.1249 mL 2.8123 mL
    40 mM 0.0844 mL 0.4218 mL 0.8437 mL 2.1092 mL
    50 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6874 mL
    60 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4061 mL
    80 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0546 mL
    100 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8437 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PCI-34051950762-95-5PCI34051PCI 34051HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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    目录号：
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