Description:IC50: 8.6 nM (singleplexed); 7.8 nM (multiplexed) USP7, also known as HAUSP, has been found to be critical in cancer progression due to its influence on the stability of the tumor suppressor p53. P022077 Inhibits ubiquitin-specific protease (USP) 7 and also inhibits the closely related deubiquitinase (DUB) USP4. In vitro: P022077 had negligible activity versus DEN1 and SENP2core over the concentration range tested, but inhibited USP7 with an IC50 of 8 μM [1]. In another study Inhibiting, USP7 with the small-molecule inhibitor P22077 attenuates the p53-dependent apoptotic pathway by destabilizing Tip60. P22077, however, is still cytotoxic, and this is partly due to destabilization of Tip60 [2]. In vivo: P022077 is currently in in-vitro investigation and no animal in vivo study is ongoing. Clinical trial: P022077 is currently in the preclinical development and no clinical trial is ongoing. References: [1] Tian X, Isamiddinova NS, Peroutka RJ, Goldenberg SJ, Mattern MR, Nicholson B, Leach C. Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev Technol. 2011;9(2):165-73. [2] Dar A, Shibata E, Dutta A. Deubiquitination of Tip60 by USP7 determines the activity of the p53-dependent apoptotic pathway. Mol Cell Biol. 2013;33(16):3309-20.
Chemical Properties
Physical Appearance
A solid
Storage
Store at 4°C
M.Wt
315.32
Cas No.
1247819-59-5
Formula
C12H7F2NO3S2
Solubility
insoluble in H2O; insoluble in EtOH; ≥14.6 mg/mL in DMSO
