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P005091 {[allProObj[0].p_purity_real_show]}

货号:A135201

P005091是一种选择性和有效的USP7抑制剂,EC50为4.2 μM。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
P005091 化学结构 CAS号:882257-11-6
P005091 化学结构
CAS号:882257-11-6
P005091 3D分子结构
CAS号:882257-11-6
P005091 化学结构 CAS号:882257-11-6
P005091 3D分子结构 CAS号:882257-11-6
规格 价格 会员价 库存 数量
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P005091 纯度/质量文件 产品仅供科研

货号:A135201 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DUB UCH USP/UBP 其他靶点 纯度
PR-619 +

Plpro, EC50: 14.2 μM

+++

UCH-L5, EC50: 12.8 μM

UCH-L3, EC50: 2.95 μM

+++

USP28, EC50: 6.24 μM

USP5, EC50: 4.90 μM

99%+
Degrasyn Bcr-Abl 98+%
VLX1570 +

DUB, IC50: ~10 μM

99%+
ML-323 ++++

USP1-UAF1, IC50: 76 nM

99%+
LDN-57444 ++++

UCH-L3, IC50: 25 μM

UCH-L1, IC50: 0.4 μM

99%+
TCID ++++

UCH-L3, IC50: 0.6 μM

98%
b-AP15 +++

UCHL5, IC50: 2.1 μM

98%
P 22077 ++

USP47, EC50: 8.74 μM

USP7, IC50: 8.6 μM

99%+
P005091 ++

USP7, EC50: 4.2 μM

USP47, IC50: 4.3 μM

99+%
IU1 ++

USP14, IC50: 4.7 μM

98%
NSC632839 +

USP2, EC50: 45 μM

USP7, EC50: 37 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

P005091 生物活性

靶点
  • USP/UBP

    USP7, EC50:4.2 μM

    USP47, IC50:4.3 μM

描述 Deubiquitylating enzymes (DUBs) antagonize the ubiquitylation of substrates by cleaving mono and polyubiquitin and thus afford an additional level of post-translational regulation. USP7 (Ubiquitin-specific protease 7) is a deubiquitinase that has activity on numerous targets, including the E3 ligase MDM2[3]. P00591 is a selective inhibitor of USP7 and USP47 activity with IC50 values of 4.2 μM and 4.3 μM[4]. P005091 stabilizes p53, inhibits cancer cell proliferation, and is active in cellular models of disease. In vitro, P005091 accelerated the degradation of the USP7 substrate HDM2 in several cancer cell lines, inhibited the growth of HCT-116 human colorectal cancer cells with an IC50 of 11 μM, and inhibited cancer cell growth synergistically with doxorubicin, etoposide, or mechlorethamine[4]. In vivo, P00591 decreased expression of PCNA and triggered cleavage of PARP and caspase-3 in a dose-dependent manner. Administration of P00591 at 10 mg/kg leaded to enhanced proliferation inhibition and apoptosis in tumor tissues in mouse colon cancer CT26 cells xenograft mice. Treatment with 10 mg/kg P005091 promoted the CD4+ and CD9+ T-cell-mediated antitumor immune response, and inhibited FOXP3+ Treg function in CT26 cells xenograft mice[5].

P005091 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human HCT116 cells Cytotoxic assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs, EC50=11 μM 24900381
Sf9 cells Function assay Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay, EC50=4.2 μM 24900381

P005091 动物研究

Dose Mice: 5 mg/kg, 10 mg/kg[3] (i.p.), 15 mg/kg - 25 mg/kg[4] (i.p.); 10 mg/kg[1] (i.v.)
Administration i.p., i.v.

P005091 参考文献

[1]22(3):345-58.

[2]3(10):789-92.

[3]Chauhan D, Tian Z, Nicholson B, Kumar KG, Zhou B, Carrasco R, McDermott JL, Leach CA, Fulcinniti M, Kodrasov MP, Weinstock J, Kingsbury WD, Hideshima T, Shah PK, Minvielle S, Altun M, Kessler BM, Orlowski R, Richardson P, Munshi N, Anderson KC. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell. 2012 Sep 11;22(3):345-58.

P005091 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.36mL

2.87mL

1.44mL

28.72mL

5.74mL

2.87mL

P005091 技术信息

CAS号882257-11-6
分子式C12H7Cl2NO3S2
分子量 348.225
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 25 mg/mL(71.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 3% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 65 mg/mL suspension

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