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USP14 Inhibitor, IU1-Calbiochem
| 半岛bd体育手机客户端 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 |
| 半岛bd体育手机客户端 类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
半岛bd体育手机客户端 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】 |
C
18H
21FN
2O
|
| 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 (IC
50= 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 (IC
50= 700 M).
A cell-permeable pyrrolylpyrrolidinyl-ethanone that inhibits the proteasome association-dependent USP14 deubiquitinase (DUB) activity in a reversible manner (IC 50= 4.7 ?M 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 ?M), 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 (IC 50= 700 ?M). |
| 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.
Nature
467,179.
|
| Legal Information【法律信息】 |
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
|
半岛bd体育手机客户端 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
|
