Search Site
Related Products
P005091Ubiquitin-specific protease 7 (USP7) inhibitor

P005091

Catalog No. A3023
Size Price Stock Qty
Evaluation Sample $28.00 In stock
10mg $80.00 In stock
50mg $250.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

P005091

Related Biological Data

P5091
HEK293T cells were treated with DMSO or P5091; crude cell extracts were labeled with indicated UbVME probe, followed by immunoblotting (IB) with indicated antibodies.

Biological Activity

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.
Targets            
IC50 4.2 μM (EC50)          

P005091 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

P005091 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 882257-11-6 SDF Download SDF
Synonyms P005091,P5091
Chemical Name 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone
Canonical SMILES CC(=O)C1=CC(=C(S1)SC2=C(C(=CC=C2)Cl)Cl)[N+](=O)[O-]
Formula C12H7Cl2NO3S2 M.Wt 348.22
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

Background

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.

Reference

Jeffrey G Marblestone. Ubiquitin Drug Discovery & Diagnostics 2009 – First Annual Conference. IDrugs. 2009; 12(12):750 – 753.