P22077
USP7 inhibitor / P22077 is a selective (tested against 23 other DUBs) inhibitor of USP7 (IC50 = 8 µM) and the closely related USP47.1,2 It destabilizes claspin, a scaffolding protein involved in regulating Chk1 kinase, a DNA damage response enzyme.2 P22077 inhibits neuroblastoma growth via induction of p53-mediated apoptosis.3 N-Myc was destabilized by P22077 inhibition of USP7 in human neuroblastoma cells.4 It was able to stabilize p53 levels in conjunction with an Mdm2 inhibitor (Nutlin-3, Cat# 10-1350) in HCT116 colorectal carcinoma cells.5
Biochemicals & reagents
1247819-59-5
1) Tian et al. (2011), Characterization of Selective Ubiquitin and Ubiquitin-like Protease Inhibitors Using a Fluorescence-Based Multiplex Assay Format; Assay Drug Dev.Technol. 9 165 2) Altun et al. (2011), Activity-based chemical proteomics accelerates inhibitor development for deubiquitinylating enzymes; Chem.Biol. 18 1401 3) Fan et al. (2013), USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis Cell Death Dis. 4 e867 4) Tavana et al. (2016), HAUSP deubiquitinated and stabilizes M-Myc in neuroblastoma; Nat.Med. 22 1180 5) Tavana et al. (2018), Targeting HAUSP in both p53 wildtype and p53-mutant tumors; Cell Cycle May 15 epub 1
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TARGET: DUB (Deubiquitinating enzyme) -- PATHWAY: DNA damage; Apoptosis inducer; Myc; Degradation; p53 -- RESEARCH AREA: Ubiquitin/Proteasome; Cell death -- DISEASE AREA: Cancer