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  1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. NSC632839

NSC632839 是一種非選擇性肽酶抑制劑,抑制 USP2USP7SENP2,EC50 分別為 45±4 μM,37±1 μM 和 9.8±1.8 μM。

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NSC632839 Chemical Structure

NSC632839 Chemical Structure

CAS No. : 157654-67-6

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10 mM * 1 mL in DMSO ¥426
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5 mg ¥388
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10 mg ¥700
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25 mg ¥1500
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Customer Review

    NSC632839 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733.  [Abstract]

    Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. Each cell lysate is analyzed by immunoblotting with anti p62 and LC3 antibodies.

    NSC632839 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733.  [Abstract]

    Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. mRFP-GFP-LC3 stable cell line is treated with 5 μM LDN or 10 μM NSC in the condition of DMSO or Torin1 respectively for 6 h. The number of LC3 puncta remarkably is raised both in LDN and NSC treatment cells compared to the control.

    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(xiàn)

    生物活性

    NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

    IC50 & Target

    EC50: 45±4 μM (USP2), 37±1 μM (USP7), 9.8±1.8 μM (SENP2)[1]

    體外研究
    (In Vitro)

    NSC 632839 抑制泛素異肽酶,如它在中微摩爾范圍內(nèi)抑制粗裂解物對 z-LRGG-AMC 裂解的能力所示。為了進(jìn)一步表征 NSC 632839 對純化酶的抑制作用,確定了其對純化的 USP2、USP7 和 SENP2 的抑制潛力,并證明 NSC 632839 不僅是 DUB 抑制劑,還是脫 SUMOylase 抑制劑。具體而言,NSC 632839 抑制 USP2、USP7 和 SENP2,EC50 值分別為 45±4 μM、37±1 μM 和 9.8±1.8 μM。重要的是,NSC 632839 在測試的濃度范圍 (1.2-150 μM) 內(nèi)不抑制報告酶 PLA2,表明報告的抑制作用對異肽酶具有選擇性。此外,NSC 632839 的異肽酶抑制活性通過觀察得到證實,即在測試的濃度范圍內(nèi)它不抑制游離 PLA2[1]。

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

    分子量

    339.86

    Formula

    C21H22ClNO

    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實驗: 

    DMSO 中的溶解度 : 4 mg/mL (11.77 mM; 超聲助溶 (<60°C); 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 2.9424 mL 14.7119 mL 29.4239 mL
    5 mM 0.5885 mL 2.9424 mL 5.8848 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(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 98.87%

    參考文獻(xiàn)
    Kinase Assay
    [1]

    In a 96-well-plate, 40 nM USP2, 40 nM USP7, or 20 nM SENP2 is preincubated with a concentration range of NSC 632839 (NCI/NIH developmental therapeutics program) or control for 30 min before supplementation with an equal volume of 60 nM Ub-PLA2/40 μM NBD C6-HPC (USP2 or 7) or 20 nM SUMO3-PLA2/40 μM NBD C6-HPC (SENP2). Relative activity of the enzymes is determined by measuring the RFU values at single time points within the initial linear range (USP, 50 min; USP7, 50 min; and SENP2, 30 min). The RFU values within the initial linear range are normalized such that isopeptidase+vehicle=0% inhibition and isopeptidase+NEM=100% inhibition. The EC50 values are determined as above. The inhibitory activity of the test compound against the reporter enzyme PLA2 is performed as described above except there is no preincubation step and the data are normalized such that free PLA2+vehicle=0% inhibition and free PLA2+EDTA=100% inhibition. PLA2 activity is determined 8 min after the addition of the reagents[1].

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

    參考文獻(xiàn)

    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(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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 2.9424 mL 14.7119 mL 29.4239 mL 73.5597 mL
    5 mM 0.5885 mL 2.9424 mL 5.8848 mL 14.7119 mL
    10 mM 0.2942 mL 1.4712 mL 2.9424 mL 7.3560 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:
    NSC632839
    目錄號:
    HY-100708
    需求量: