| 货号 | 11324-1mg |
| 描述 | Proteasome-associated deubiquitinases (DUBs) release ubiquitin from proteasome-targeted ubiquitinated proteins, regenerating free ubiquitin.1 b-AP15 is an inhibitor of ubiquitin-specific-processing protease 14 (USP14) and ubiquitin carboxyl-terminal hydrolase isozyme L5 (UCHL5), two proteasome-associated DUBs.2 It inhibits DUB activity in purified 19S proteasomes with an IC50 value of 2.1 µM.2 It exhibits little or no activity against several other DUBs.2 Through its effects on USP14 and UCHL5, b-AP15 blocks tumor progression in vivo in mice and prevents organ infiltration in mouse models of myeloid leukemia.2,3 b-AP15 also renders tumor cells sensitive to TNF-mediated apoptosis by natural killer and T cells.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Zhang, W. and Sidhu, S.S. Development of inhibitors in the ubiquitination cascade. FEBS Letters 588(2), 356-367 (2014). 2.DArcy, P.,Brnjic, S.,Olofsson, M.H., et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy. Nature Medicine 17(12), 1636-1640 (2011). 3.Tian, Z.,DArcy, P.,Wang, X., et al. A novel small molecule inhibitor of deubiquitylating enzyme USP14 and UCHL5 induces apoptosis in multiple myeloma and overcomes bortezomib resistance. Blood 123(5), 706-716 (2014). 4.Sarhan, D.,Wennerberg, E.,DArcy, P., et al. A novel inhibitor of proteasome deubiquitinating activity renders tumor cells sensitive to TRAIL-mediated apoptosis by natural killer cells and T cells. Cancer Immunol.Immunother. 62(8), 1359-1368 (2013). | |
| 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 | 419.4 |
| 分子式 | C22H17N3O6 |
| CAS号 | 1009817-63-3 |
| 稳定性 | ≥ 2 years |
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