WP1130
货号:
15227-1mg 基本售价:
350.0 元 规格:
1 mg
产品信息
概述货号 | 15227-1mg |
描述 | Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into two subgroups: ubiquitin-specific proteases (USPs) and ubiquitin-specific COOH-terminal hydrolases (UCHs). Recent evidence suggests that several DUBs are activated in tumor cells and many contribute to a transformed phenotype.1 WP1130 is a second-generation tyrphostin derivative that inhibits the deubiquitinase activity of USP9x, USP5, USP14, and UCH37.2,1 At 5 μM, WP1130-mediated inhibition of tumor-activated DUBs induces a rapid accumulation of protein-ubiquitin conjugates, resulting in the formation of aggresomes and apoptosis in a variety of tumor cells.1 Through this mechanism, WP1130 has been shown to downregulate the antiapoptotic proteins Bcr/Abl and Jak2 and to upregulate the proapoptotic proteins MCL-1 and p53.1 |
别名 | Degrasyn; |
性能供应商 | Cayman |
应用文献 |
1.Kapuria, V.,Peterson, L.F.,Fang, D., et al. Deubiquitinase inhibition by small-molecule WP1130 triggers aggresome formation and tumor cell apoptosis. Cancer Research 70(22), 9265-9276 (2010). 2.Bartholomeusz, G.A.,Talpaz, M.,Kapuria, V., et al. Activation of a novel Bcr/Abl destruction pathway by WP1130 induces apoptosis of chronic myelogenous leukemia cells. Blood 109(8), 3470-3478 (2007).
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运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 384.3 |
分子式 | C19H18BrN3O |
CAS号 | 856243-80-6 |
稳定性 | ≥ 2 years |
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