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| 化学名: | | | 英語化学名: | P-5091 | | 别名: | 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitro-2-thienyl]ethanone;P5091, >=98%;1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone;Ethanone, 1-[5-[(2,3-dichlorophenyl)thio]-4-nitro-2-thienyl]-;1-[5-[(2,3-Dichlorophenyl)thio]-4-nitro-2-thienyl]-ethanone P005091;P 005091;P 5091;P005091 | | CAS番号: | 882257-11-6 | | 分子式: | C12H7Cl2NO3S2 | | 分子量: | 348.22 | | EINECS: | | | カテゴリ情報: | Inhibitors | | Mol File: | 882257-11-6.mol |  |
| 沸点 | 452.4±45.0 °C(Predicted) | | 比重(密度) | 1.60±0.1 g/cm3(Predicted) | | 貯蔵温度 | 2-8°C | | 溶解性 | DMSO: soluble10mg/mL, clear | | 外見 | powder | | 色 | light yellow to dark yellow | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| 主な危険性 | T | | Rフレーズ | 25 | | Sフレーズ | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| | P-5091 Usage And Synthesis |
| 説明 | P5091 (882257-11-6) is a selective inhibitor of the ubiquitin-specific protease USP7 ( IC50=4.2 μM).1,2 Induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.1?P5091 displays antiangiogenic activity in vivo.2?Cell permeable | | 使用 | P005091 is a selective dual inhibitor of the cancer-related deubiquitylating proteases USP7 and USP47. | | 使用 | P5091 has been used:
- as a ubiquitin specific peptidase 47 (USP47) inhibitor in 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to evaluate the cellular viability of MCF-10A cells
- as a USP7 inhibitor to study the regulatory role for USP7 on inflammasome activation
- as USP7 inhibitor in drug susceptibility assays to study its effect on bone marrow?resident tumor cells (BMRTCs)/ circulating tumor cells (CTCs)
| | Biochem/physiol Actions | P5091 plays an important role in ovarian cancer, as it can prevent the growth of cells and can promote necrosis and apoptosis. | | 参考文献 | 1) Chauhan et al. (2012), A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance; Cancer Cell, 22 345
2) Weinstock et al. (2012), Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47; ACS Med. Chem. Lett., 3 789 |
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