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  1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. USP7-IN-1

USP7-IN-1 是一種選擇性的,可逆的泛素蛋白特異性蛋白酶 (USP7) 抑制劑,IC50 值為 77 μM,可用于癌癥研究。

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USP7-IN-1 Chemical Structure

USP7-IN-1 Chemical Structure

CAS No. : 1381291-36-6

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10 mM * 1 mL in DMSO ¥2027
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1 mg ¥998
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5 mg ¥2163
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10 mg ¥3113
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25 mg ¥4900
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Customer Review

    USP7-IN-1 purchased from MCE. Usage Cited in: Nat Commun. 2019 Jan 24;10(1):411.  [Abstract]

    Immunoblot analysis of lysates from Huh7 cells treated with Usp7-IN-1 at indicated concentrations for 24 h.

    查看 Deubiquitinase 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.

    IC50 & Target

    IC50: 77 μM (USP7)[1]

    體外研究
    (In Vitro)

    USP7-IN-1 (Example 2) is a selective and reversible inhibitor of USP7, with an IC50 of 77 μM, and shows no inhibition of USP8, USP5, Uch-L1, Uch-L3 or caspase 3. USP7-IN-1 inhibits the proliferation of HCT116 cells, with a GI50 of 67 μM[1].

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

    分子量

    425.91

    Formula

    C23H24ClN3O3

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    運輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗: 

    DMSO 中的溶解度 : 100 mg/mL (234.79 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.3479 mL 11.7396 mL 23.4791 mL
    5 mM 0.4696 mL 2.3479 mL 4.6958 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗:

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用
    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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.87 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

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.87 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 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實驗過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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 2%。
    方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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)給藥周期超過半月以上,請謹慎選擇該方案。
    請確保第一步儲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
    參考文獻
    Kinase Assay
    [1]

    USP7 is diluted in USP buffer (50 mM Tris HCl; 0.5 mM EDTA (Ethylenediaminetetraacetic acid); 5 mM DTT; 0.01 % Triton X-100; Bovine Serum Albumin 0.05 mg/mL pH7.6). Compounds stocks (10 mM) are stored at -20°C in DMSO. Compounds (including USP7-IN-1) are tested at different concentrations: from 200 μM to 91 nM. Reactions are performed as duplicates in Black 384 well plates (10 μL final reaction volume). The substrate concentration for USP7 is 300 nM Ub-AMC. The concentrations of the enzyme (USP7) in specificity assays is 100 pM. The concentrations are determined in order to perform specificity assays under initial velocities at fixed substrate concentration. Compounds are pre-incubated with enzymes for 30 minutes at 25°C. Reactions are initiated by addition of substrate to the plates containing the enzymes (+/- compounds) diluted in assay buffer. Reactions are incubated for 60 minutes at 37°C. Reactions are stopped by adding acetic acid (100 mM final). Readings are performed on a Pherastar Fluorescent Reader. λ Emission 380 nm; λ Excitation = 460 nm. Data (mean values +/- standard deviation) are analyzed as % of control (no compound) and plotted as percentage versus the Log of the compound concentration using GraphPad. Data are fitted to a sigmoidal model (variable slope)[1].

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

    Cell Assay
    [1]

    HCT116 colon cancer cells are maintained in Mc Coy's 5A medium containing 10% FBS, 3 mM glutamine and 1 % penicillin/streptomycin. Cells are incubated at 37°C in a humidified atmosphere containing 5% CO2. Cell viability is assayed using the MTS technique in 96-well culture plates. MTS (3-(4,5-dimethyl-thiazol-2-yl)-5-(3-carboxy- methoxyphenyl)-2-(4-sulfophenyl)-2H-tetra-zolium) is a MTT-derived tetrazolium that is reduced in metabolically active cells into a soluble, cell-permeant formazan. The amount of formazan, detected by its absorbance at 492 nm is proportional to the number of living, metabolically active cells. 103 HCT116 cells are seeded per well. 24 hours later, the medium is changed and the cells treated in triplicate with the concentrations of each compound from 100 μM to 50 nM. The compounds (including USP7-IN-1) are diluted in 100% DMSO, whose final concentration on cells is kept at 0.5%. Cells are incubated with the compounds for 72 hours, and their viability then assayed by the addition of MTS for 2 hours. Absorbance at 492 nm is measured directly from the 96-well culture plates. GI50 (Growth Inhibition 50) concentrations for each compound are calculated using a sigmoidal variable slope fit. Values represent mean of three independent experiments[1].

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

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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 2.3479 mL 11.7396 mL 23.4791 mL 58.6978 mL
    5 mM 0.4696 mL 2.3479 mL 4.6958 mL 11.7396 mL
    10 mM 0.2348 mL 1.1740 mL 2.3479 mL 5.8698 mL
    15 mM 0.1565 mL 0.7826 mL 1.5653 mL 3.9132 mL
    20 mM 0.1174 mL 0.5870 mL 1.1740 mL 2.9349 mL
    25 mM 0.0939 mL 0.4696 mL 0.9392 mL 2.3479 mL
    30 mM 0.0783 mL 0.3913 mL 0.7826 mL 1.9566 mL
    40 mM 0.0587 mL 0.2935 mL 0.5870 mL 1.4674 mL
    50 mM 0.0470 mL 0.2348 mL 0.4696 mL 1.1740 mL
    60 mM 0.0391 mL 0.1957 mL 0.3913 mL 0.9783 mL
    80 mM 0.0293 mL 0.1467 mL 0.2935 mL 0.7337 mL
    100 mM 0.0235 mL 0.1174 mL 0.2348 mL 0.5870 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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    Inquiry Information

    產(chǎn)品名稱:
    USP7-IN-1
    目錄號:
    HY-16709
    需求量: