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IU1

Catalog No.
A4002
Usp14 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$60.00
In stock
10mg
$50.00
In stock
50mg
$200.00
In stock
100mg
$360.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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 IC50 ranging 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

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

Chemical Properties

Physical AppearanceA solid
StorageStore at 4°C
M.Wt300.37
Cas No.314245-33-5
FormulaC18H21FN2O
SynonymsUsp14 inhibitor
Solubility≥10.9 mg/mL in DMSO, ≥81.8 mg/mL in EtOH,insoluble in H2O
Chemical Name1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone
SDFDownload SDF
Canonical SMILESCC1=CC(=C(N1C2=CC=C(C=C2)F)C)C(=O)CN3CCCC3
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description IU1 is a cell-permeable, reversible and selective proteasome inhibitor of human USP14 with IC50 of 4.7 μM.
Targets USP14          
IC50 4.7 μM          

Quality Control

Chemical structure

IU1