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P005091

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Chemical Structure| 882257-11-6 同义名 : -
CAS号 : 882257-11-6
货号 : A135201
分子式 : C12H7Cl2NO3S2
纯度 : 99+%
分子量 : 348.225
MDL号 : MFCD00123202
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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

生物活性
靶点

  • USP/UBP

    USP47, IC50:4.3 μM

    USP7, EC50:4.2 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].
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
实验方案
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
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.