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

Tubacin 是一種有效的,選擇性的 HDAC6 抑制劑,IC50 值為 4 nM,大約是對(duì) HDAC1 的 350 倍。Tubacin 還抑制 MBLAC2

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Tubacin Chemical Structure

Tubacin Chemical Structure

CAS No. : 537049-40-4

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10 mM * 1 mL in DMSO ¥3811
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1 mg ¥900
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10 mg ¥4080
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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.

    查看 Beta-lactamase 亞型特異性產(chǎn)品:

    查看 HDAC 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 EC50
    2.5 μM
    Compound: 38
    Inhibition of HDAC-6 in human A549 cells assessed as induction of alpha-tubulin acetylation after 20 hrs by cytoblot analysis
    Inhibition of HDAC-6 in human A549 cells assessed as induction of alpha-tubulin acetylation after 20 hrs by cytoblot analysis
    10.1039/C1MD00199J
    A549 EC50
    2.9 μM
    Compound: Tubacin
    Inhibition of HDAC6 in human A549 cells assessed as induction of alpha-tubulin acetylation by fluorescence microscopy
    Inhibition of HDAC6 in human A549 cells assessed as induction of alpha-tubulin acetylation by fluorescence microscopy
    [PMID: 16408003]
    HeLa IC50
    2.9 μM
    Compound: Tubacin
    Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay
    Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay
    [PMID: 25454270]
    HeLa IC50
    2.9 μM
    Compound: Tubacin
    Inhibition of HDAC6 in human HeLa cells using acetyl tubulin as substrate assessed as Ac-Lys accumulation in nuclear histones after 6 hrs by immunofluorescence assay
    Inhibition of HDAC6 in human HeLa cells using acetyl tubulin as substrate assessed as Ac-Lys accumulation in nuclear histones after 6 hrs by immunofluorescence assay
    [PMID: 23964961]
    體外研究
    (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 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 100 mg/mL (138.53 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn):

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.46 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.46 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.54%

    參考文獻(xiàn)
    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.

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲(chǔ)備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
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      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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    產(chǎn)品名稱:
    Tubacin
    目錄號(hào):
    HY-13428
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