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IU1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IU1图片
CAS NO:314245-33-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议

产品介绍
IU1 是一种特殊的 Usp14 抑制剂,IC50 为 4-5 μM。
Cas No.314245-33-5
别名Usp14 inhibitor
化学名1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone
Canonical SMILESCC1=CC(=C(N1C2=CC=C(C=C2)F)C)C(=O)CN3CCCC3
分子式C18H21FN2O
分子量300.37
溶解度≥ 10.9 mg/mL in DMSO, ≥ 81.8 mg/mL in EtOH
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IU1 is a potent and selective small-molecule inhibitor of Usp14, a proteasome-associated deubiquitinating enzyme in habiting the degradation of ubiquitin-protein conjugates, with the inhibition constant IC50ranging from 4 to 5 μM. Structural analysis reveals IU1 is an active-site-directed thiol protease inhibitor that binds to the activated form of Usp14 preventing it docking on the proteasome in a rapid but reversible manner. According to the results of previous studies, it has shown that IU1 failed to inhibit Usp14 in the absence of proteasomes as well as eight deubiquitinating enzymes (DUBs) of human origin and Ub-AMC hrolysis by proteasomes lacking Usp14.

Reference

[1].Byung-Hoon Lee, Min Jae Lee, Soyeon Park, Dong-Chan Oh, Suzanne Elsasser, Ping-Chung Chen, Carlos Gartner, Nevena Dimova, John Hanna, Steven P. Gygi, Scott M. Wilson, Randall W. King and Daniel Finley. Enhancement of proteasome activity by a small-molecule inhibitor of Usp14. Nature. 2010; 467(7312): 179-184