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DUB 抑制剂 VI，P22077-Calbiochem
DUB Inhibitor VI, P22077-Calbiochem
| 产品编号： | 4156681 |
| 规格： | The DUB Inhibitor VI, P22077 controls the biological activity of DUB. This small molecule/inhibitor is primarily used for Protease Inhibitors applications. |
| 包装规格： | 25 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
DUB 抑制剂 VI，P22077-Calbiochem
DUB Inhibitor VI, P22077-Calbiochem
P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone, USP7 Inhibitor II, USP47 Inhibitor II
USP7 Inhibitor II, USP47 Inhibitor II, P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C12H7F2NO3S2 |
| Molecular weight | 315.32 |
| MDL number | MFCD22580421 |
| General description【一般描述】 | A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50 = 8.01 & 8.74 µM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 (Cat. No. 662141) targets (IC50 >50 µM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 µM; 0.5 to 20 h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains. A cell-permeable thiophenylethanone compound that acts a direct, reversible, and selective inhibitor of deubiquitylating enzymes (DUBs) USP7 and USP47 (IC50 = 8.01 & 8.74 µM, respectively). Exhibits only a minimal effect on other DUBs and proteases (>25 µM). Also shown to block UCH-L5 activity in HEK293T cell extracts, but not in intact cells. Stabilizes p53, HDM2, and p21 levels in HEK293T and HCT-116 cells and induces growth arrest (50% cytotoxicity concentration; CC50 = 16.6 and 7.83 µM). Note: A pan-DUB selective inhibitor PR-619 (Cat. No. 662141) is also available. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Altun, M., et al. 2011. Chem. Biol.18, 1401. Tian, X., et al. 2011. Assay Drug Dev. Technol.9, 165. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O |
| packaging【包装】 | 25 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
