Chemical Name: 1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]-ethanone
Biological ActivityP 22077 is an inhibitor of ubiquitin-specific protease (USP) 7 (EC50 = 8.6 μM); also inhibits the closely related deubiquitinase (DUB) USP47. Demonstrates downstream inhibition of HDM2 and claspin in vitro. Inhibits USP7-mediated p53 deubiquitination. Blocks deubiquitination of Tip60 (KAT5) histone lysine acetyltransferase.
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Deubiquitination of Tip60 by USP7 determines the activity of the p53-dependent apoptotic pathway.
Dar et al.
Mol.Cell Biol., 2013;33:3309
Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes.
Altun et al.
Deubiquitylase, deSUMOylase, and deISGylase activity microarrays for assay of substrate preference and functional modifiers.
Loch et al.
Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format.
Tian et al.
Assay Drug Dev.Technol., 2011;9:165
Citations for P 22077
The citations listed below are publications that use Tocris products. Selected citations for P 22077 include:
3 Citations: Showing 1 - 3
USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin.
Authors: Ji Et al.
Nat Commun 2019;10:4184
USP7 is a SUMO deubiquitinase essential for DNA replication.
Authors: Lecona Et al.
Nat Struct Mol Biol 2016;23:270
USP7 cooperates with SCML2 to regulate the activity of PRC1.
Authors: Lecona Et al.
Pharmacol Res Perspect 2015;35:1157
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P22077 was seen to induce (tumor) cell death with EC50 values in the low micromolar range. P22077 inhibition exhibited changes in ubiquitylated protein levels that are distinct from the broad specificity inhibitor.
HEK293T cells stably expressing the STF-Luc reporter were pretreated with increasing amounts of USP7 inhibitors P22077