1. Cell Cycle/DNA Damage Epigenetics Anti-infection
  2. Beta-lactamase HDAC Virus Protease
  3. Tubacin

Tubacin 是一种有效的,选择性的 HDAC6 抑制剂,IC50 值为 4 nM,大约是对 HDAC1 的 350 倍。Tubacin 还抑制 MBLAC2

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Tubacin Chemical Structure

Tubacin Chemical Structure

CAS No. : 537049-40-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3811
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1 mg ¥900
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5 mg ¥2400
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10 mg ¥4080
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100 mg   询价  

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Customer Review

    Tubacin purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jun;114:108805.  [Abstract]

    Western blot is used for the detection of VEGFA and Hsp-90 with or without the treatment of Tubacin.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).

    IC50 & Target[1]

    HDAC6

    4 nM (IC50)

    HDAC3

    1.27 μM (IC50)

    HDAC8

    1.27 μM (IC50)

    HDAC1

    1.40 μM (IC50)

    HDAC5

    3.35 μM (IC50)

    HDAC10

    3.71 μM (IC50)

    HDAC11

    3.79 μM (IC50)

    HDAC9

    4.31 μM (IC50)

    HDAC2

    6.27 μM (IC50)

    HDAC7

    9.70 μM (IC50)

    HDAC4

    17.30 μM (IC50)

    体外研究
    (In Vitro)

    Tubacin preferentially induces α-tubulin hyperacetylation at a concentration of 2.5 μM, and induces α-tubulin acetylation at 5 μM and protects prostate cancer (LNCaP) cells from hydrogen peroxide-induced death at 8 μM via peroxiredoxin acetylation[1]. Tubacin (2.5 and 5 μM) specifically induces acetylation of α-tubulin in MM cells. Tubacin significantly inhibits both drug-sensitive and drug-resistant MM cell growth, with IC50 5-20 μM at 72 h. Tubacin also induces apoptosis by activation of caspases. Moreover, Tubacin inhibits binding of HDAC6 with dynein, and it induces significant accumulation of polyubiquitinated proteins, when combined with bortezomib. Tubacin and bortezomib induce synergistic antitumor activity in MM cell lines, and inhibits paracrine MM Cell Growth. Tubacin (5 μM) synergistically enhances bortezomib-induced cytotoxicity in patient MM cells without cytotoxicity to PBMCs[2]. Tubacin can concentration-dependently inhibits JEV-induced cytopathic effect and apoptosis, as well as reduces virus yield in human cerebellar medulloblastoma cells. The IC50 of virus yield is 0.26 μM for Tubacin. Tubacin also meaningfully blocks the production of intracellular infectious virus particles, with an IC50 of 1.52 μM. Tubacin induces the hyperacetylation of a HDAC6 substrate Hsp90 and reduces the interaction of Hsp90 with JEV NS5 protein[3].

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

    分子量

    721.86

    Formula

    C41H43N3O7S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (138.53 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.3853 mL 6.9266 mL 13.8531 mL
    5 mM 0.2771 mL 1.3853 mL 2.7706 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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

    动物实验:

    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 (3.46 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。

      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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.46 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,此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中,混合均匀。

    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

    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: 99.54%

    参考文献
    Cell Assay
    [3]

    HDAC inhibitors TSA, VPA, tubacin, and TBSA are used in the assay. Cytotoxicity of HDACi to TE671 and BHK-21 cells is evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. 5 × 104 cells per well are seeded in 96-well plates and then treated with the indicated concentration of each HDACi. After 48-h of treatment, 25 μL of MTT solution (5 mg/mL) is added to each well and incubated at 37 °C with 5% CO2 for 3 h. After three washings with phosphate buffer saline (PBS), 100 μL DMSO is added into each well for dissolving formazan crystals. OD570−630 is measured by micro-ELISA reader and survival rate are calculated to indicate suppressive effects of each HDACi on the survival of TE671 and BHK-21 cells. Survival rate (%) = ((Acontrol − Aexperiment)/Acontrol) × 100%. 50% cytotoxic concentration (CC50) values are calculated by computer program[3].

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

    参考文献

    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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.3853 mL 6.9266 mL 13.8531 mL 34.6328 mL
    5 mM 0.2771 mL 1.3853 mL 2.7706 mL 6.9266 mL
    10 mM 0.1385 mL 0.6927 mL 1.3853 mL 3.4633 mL
    15 mM 0.0924 mL 0.4618 mL 0.9235 mL 2.3089 mL
    20 mM 0.0693 mL 0.3463 mL 0.6927 mL 1.7316 mL
    25 mM 0.0554 mL 0.2771 mL 0.5541 mL 1.3853 mL
    30 mM 0.0462 mL 0.2309 mL 0.4618 mL 1.1544 mL
    40 mM 0.0346 mL 0.1732 mL 0.3463 mL 0.8658 mL
    50 mM 0.0277 mL 0.1385 mL 0.2771 mL 0.6927 mL
    60 mM 0.0231 mL 0.1154 mL 0.2309 mL 0.5772 mL
    80 mM 0.0173 mL 0.0866 mL 0.1732 mL 0.4329 mL
    100 mM 0.0139 mL 0.0693 mL 0.1385 mL 0.3463 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.

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    产品名称:
    Tubacin
    目录号:
    HY-13428
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