CAS NO: | 314245-33-5 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
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 SMILES | CC1=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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 |