|P005091Ubiquitin-specific protease 7 (USP7) inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Description||P5091(P005091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.|
|IC50||4.2 μM (EC50)|
|Cas No.||882257-11-6||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at 4°C|
|General tips||For 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.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
P005091 is a selective, potent inhibitor of USP7 deubiquitylating activity, which is demonstrated to downregulate claspin and phosphorylation of the DNA checkpoint kinase Chk1, and to synergize with genotoxic agents. USP7, known as herpes-associated-ubiquitin-specificprotease (HAUSP), is a deubiquitylating enzyme that regulates the levels of the oncoprotein HDM2 and its substrate, the tumor suppressor p53. P005091 accelerated the degradation of HDM2, while analogs of the compound induced dose- and time-dependent increases in the protein levels of p53 and p21.What’s more,P005091 induced apoptosis in numerous cancer cell lines, including both p53+/+ and p53-mutant cancer cell lines.
Jeffrey G Marblestone. Ubiquitin Drug Discovery & Diagnostics 2009 – First Annual Conference. IDrugs. 2009; 12(12):750 – 753.