P005091
货号：
15224-50mg 基本售价：
5236.0 元 规格：
50 mg
产品信息
概述| 货号 | 15224-50mg |
| 描述 | Ubiquitin-specific proteases (USP/UBP) remove ubiquitin from proteins, sparing them from degradation by the proteasome. USP7 is a cysteine protease associated with prostate cancer that selectively deubiquitylates HDM2, the ubiquitin E3 ligase for the tumor suppressor p53. P005091 is a trisubstituted thiophene that inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50s = > 100 μM).1,2 P005091 has been shown to accelerate the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 = 11 μM) and to inhibit the growth of HCT116 human colorectal cancer cells (EC50 = 11 μM) synergistically with doxorubicin, etoposide, or mechlorethamine.1In vivo, 10 mg/kg P005091 prolongs survival and reduces tumor growth in mice bearing human multiple myeloma and B cell leukemia xenografts.1 |
| 别名 | P5091; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Chauhan, D.,Tian, Z.,Nicholson, B., et al. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell 22(3), 345-358 (2012).
2.Weinstock, J.,Wu, J.,Cao, P., et al. Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47. ACS Med.Chem.Lett. 3, 789-792 (2012).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 348.2 |
| 分子式 | C12H7Cl2NO3S2 |
| CAS号 | 882257-11-6 |
| 稳定性 | ≥ 2 years |
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