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USP14 Inhibitor, IU1-Calbiochem
| 产品编号： | 4170435 |
| 规格： | The USP14 Inhibitor, IU1 controls the biological activity of USP14. This small molecule/inhibitor is primarily used for Cell Structure applications. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
USP14 Inhibitor, IU1-Calbiochem
1-(1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl)-2-(pyrrolidin-1-yl)ethanone, 1-(1-(4-Fluorophenyl)-2,5-dimethylpyrrol-3-yl)-2-pyrrolidin-1-ylethanone, Ubiquitin Specific Protease 14 Inhibitor, DUB Inhibitor IX
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H21FN2O |
| Molecular weight | 300.37 |
| MDL number | MFCD01917473 |
| General description【一般描述】 | A cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC50 = 4.7 M against Ub-AMC hydrolysis), likely by targeting USP14 active site thiol, while exhibiting little or no activity toward 8 other DUBs (<10% inhibition of IsoT, UCH37/UCH-L5, BAP1, UCH-L1, UCH-L3, USP2, USP7, and USP15 at 17 M). Shown to downregulate tau, TDP-43, ATXN3, GFAP, and free Ub levels in MEF cultures in a dose- (25 to 100 M), time-, and USP14-dependent manner. Effectively protects HEK293 cells from menadione toxicity (90% vs. 40% viability after 4 h 100 M menadione treatment, respectively, with or without 50 M IU1 pretreatment) by reducing the built-up of oxidized proteins. USP14-catalyzed trimming of protein surface polyubiquitin chains rescues proteasome-bound proteins from proteolytic degradation and thereby prevents the depletion of free ubiquitin pool in cells. Comparing to b-AP15 (Cat. No. 662140), IU1 does not inhibit UCH37/UCH-L5 (IC50 = 700 M). A cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC50 = 4.7 µM against Ub-AMC hydrolysis), exhibiting little or no activity toward 8 other DUBs. Shown to downregulate tau, TDP-43, ATXN3, GFAP, and free Ub levels in MEF cultures in a dose- (25 to 100 µM), time-, and USP14-dependent manner. USP14-catalyzed trimming of protein surface polyubiquitin chains rescues proteasome-bound proteins from proteolytic degradation and thereby prevents the depletion of free ubiquitin pool in cells. Comparing to b-AP15 (Cat. No. 662140), IU1 does not inhibit UCH37/UCH-L5 (IC50 = 700 µM). |
| Warning【警告】 | Toxicity: Regulatory Review (Z) |
| 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】 | Lee, B.H., et al. 2010. Nature467, 179. |
| 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】 | ≥90% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | beige |
| solubility【溶解性】 | DMSO: 50 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 10 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 |
