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

P005091  (Synonyms: P5091)

目录号: HY-15667 纯度: 99.90%
COA 产品使用指南 技术支持

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.

Customer Review

P005091 相关抗体

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.

    查看 Deubiquitinase 亚型特异性产品:

    查看所有亚型
    USP1 USP2 USP7 USP8 USP10 USP30 UCHL1

    • 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)
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 IC50
    11 μM
    Compound: 1, P-005091
    Cytotoxicity against human HCT116 cells after 72 hrs
    Cytotoxicity against human HCT116 cells after 72 hrs
    		[PMID: 24900381]
    Sf9 IC50
    4.2 μM
    Compound: 1, P-005091
    Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay
    Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay
    		[PMID: 24900381]
    体外研究
    (In Vitro)

    P005091 是一种三取代噻吩类化合物，其二氯苯硫基、硝基和乙酰基取代基可介导抗 USP7 活性。P005091 对 USP7 表现出强效、特异且选择性的去泛素化活性，而对其他测试的去泛素化酶 (DUBs) 或半胱氨酸蛋白酶家族无抑制作用 (EC50 > 100 mM)。P005091 能以浓度依赖性方式抑制 HA-UbVME 对 USP7 的标记，并以剂量依赖性方式抑制 USP7 介导的高分子量多聚泛素链的切割。此外，P005091 特异性抑制 USP7 (而非 USP2 或 USP8) 介导的 K48 连接多聚泛素链的切割。
    P005091 通过抑制 USP7 诱导 HDM2 多聚泛素化并加速其降解。在 MM 细胞中，P005091 能抑制 USP7 的去泛素化活性，且不阻断蛋白酶体活性。P005091 可抑制 MM 细胞生长并克服硼替佐米耐药性，对多种 MM 细胞系 (包括对常规治疗药物地塞米松 (MM.1R)、阿霉素 (Dox-40) 和美法仑 (LR5) 耐药的细胞系) 均产生剂量依赖性的细胞活力下降 (IC50 范围为 6-14 μM)，并能克服骨髓基质细胞诱导的 MM 细胞生长。
    P005091 可降低 HDM2 和 HDMX 水平，同时上调 p53 和 p21 表达。总体而言，P005091 诱导的细胞毒性部分通过 HDM2-p21 信号轴介导，虽然 p53 在 P005091 处理后表达上调，但其细胞毒活性不依赖于 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)

    在动物肿瘤模型研究中，P005091 表现出良好的耐受性，能有效抑制肿瘤生长并延长生存期。当 P005091 与来那度胺 (lenalidomide)、组蛋白去乙酰化酶抑制剂 SAHA 或地塞米松 (dexamethasone) 联用时，可产生协同抗多发性骨髓瘤 (MM) 活性[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
    细胞实验： 

    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

    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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.92%

    COA (290 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 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
    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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