2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. P005091

P005091  (Synonyms: P5091)

目录号: HY-15667 纯度: 99.85%
COA 产品使用指南

摩尔计算器

P005091 是一种有效的，选择性的泛素特异性蛋白酶7 (USP7) 抑制剂，EC50 值为 4.2 μM。

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P005091 Chemical Structure

P005091 Chemical Structure

CAS No. : 882257-11-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥825
In-stock
1 mg ￥300
In-stock
5 mg ￥750
In-stock
10 mg ￥1083
In-stock
50 mg ￥3500
In-stock
100 mg ￥5413
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

P005091 相关抗体

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Top Publications Citing Use of Products

    P005091 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Nov 15;38(1):468.   [Abstract]

    DU145 and VCaP cells are treated with the USP7 inhibitor P5091 for 24 h, and the protein levels of USP7 and PLK1 are assessed by immunoblotting.

    P005091 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Nov 15;38(1):468.   [Abstract]

    DU145 and VCaP cells are treated with the USP7 inhibitor P5091 for 24 h, and the protein levels of USP7 and PLK1 are assessed by immunoblotting.

    P005091 purchased from MCE. Usage Cited in: Mol Carcinog. 2019 Jan;58(1):42-54.  [Abstract]

    Treatment with P5091 increases the cleavage of CASP9, CASP3, and PARP. ESCC cells Kyse450, Kyse510 and Kyse30 are treated with P5091 for 72 h and cell lysates are assessed by western blotting with specific antibodies against cleaved CASP9, CASP3, or PARP. GAPDH is used as a control.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.

    IC50 & Target

    EC50: 4.2 μM (USP7)
    体外研究
    (In Vitro)

    P005091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P005091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P005091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P005091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P005091. Moreover, P005091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P005091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P005091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P005091 inhibits growth in MM cells and overcomes bortezomib-resistance. P005091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6-14 μM). P005091 overcomes bone marrow stromal cell-induced growth of MM Cells. P005091 decreases HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, P005091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P005091 treatment, the cytotoxic activity of P005091 is not dependent on p53[1].

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

    P005091 相关抗体:
    体内研究
    (In Vivo)

    In animal tumor model studies, P005091 is well tolerated, inhibits tumor growth, and prolongs survival. Combining P005091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggers synergistic anti-MM activity[1].

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

    348.22

    Formula

    C12H7Cl2NO3S2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    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: 

    1-Methyl-2-pyrrolidinone 中的溶解度 : 100 mg/mL (287.17 mM; 超声助溶)

    DMSO 中的溶解度 : 25 mg/mL (71.79 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 2.8717 mL 14.3587 mL 28.7175 mL
    5 mM 0.5743 mL 2.8717 mL 5.7435 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： 4% NMP    3% Tween-80    20% PEG400    73% ddH2O

      Solubility: 8 mg/mL (22.97 mM); 悬浊液; 超声助溶

    • 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 (7.18 mM); 悬浊液; 超声加热助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      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: 99.92%

    COA (197 KB) LCMS (121 KB)

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

    Recombinant enzymes in 20 mM Tris-HCl (pH 8.0), 2 mM CaCl2, and 2 mM β-mercaptoethanol are incubated with dose ranges of P005091 for 30 min in a 96-well plate before the addition of Ub-PLA2 and NBD C6-HPC or Ub-EKL and EKL substrate. The liberation of a fluorescent product within the linear range of the assay is monitored using a Perkin Elmer Envision fluorescence plate reader. Vehicle (2% [v/v] DMSO) and 10 mM N-ethylmaleimide (NEM) are included as controls.

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

    For the animal study, P005091 is dissolved in 4% NMP(N-methyl-2-Pyrrolidone), 4% Tween-80, and 92% Milli-Q water at a final concentration of 2 mg/mL. The human plasmacytoma xenograft model is performed as previously described. CB-17 SCID-mice are subcutaneously inoculated with MM.1S, ARP-1, or RPMI-8226 cells in 100 μL of serum free RPMI-1640 medium. When tumors are measurable (100-180 mm3), mice are randomized into treatment groups. In the SCID-hu model, human fetal bone grafts are subcutaneously implanted into SCID mice. Four weeks after bone implantation, INA-6 cells are injected directly into the fetal bone implant in SCID mice; and as a measure of tumor burden, mouse sera samples are analyzed for shIL-6R by ELISA. Upon detection of shIL-6R, mice are treated with vehicle or P005091, and mouse serum is analyzed for alterations in shIL-6R levels.

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

    P005091 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-Methyl-2-pyrrolidinone 1 mM 2.8717 mL 14.3587 mL 28.7175 mL 71.7937 mL
    5 mM 0.5743 mL 2.8717 mL 5.7435 mL 14.3587 mL
    10 mM 0.2872 mL 1.4359 mL 2.8717 mL 7.1794 mL
    15 mM 0.1914 mL 0.9572 mL 1.9145 mL 4.7862 mL
    20 mM 0.1436 mL 0.7179 mL 1.4359 mL 3.5897 mL
    25 mM 0.1149 mL 0.5743 mL 1.1487 mL 2.8717 mL
    30 mM 0.0957 mL 0.4786 mL 0.9572 mL 2.3931 mL
    40 mM 0.0718 mL 0.3590 mL 0.7179 mL 1.7948 mL
    50 mM 0.0574 mL 0.2872 mL 0.5743 mL 1.4359 mL
    60 mM 0.0479 mL 0.2393 mL 0.4786 mL 1.1966 mL
    1-Methyl-2-pyrrolidinone 80 mM 0.0359 mL 0.1795 mL 0.3590 mL 0.8974 mL
    100 mM 0.0287 mL 0.1436 mL 0.2872 mL 0.7179 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:

    P005091882257-11-6P5091P 005091P-005091P 5091P-5091DeubiquitinaseDUBsInhibitorinhibitorinhibit

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