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Description

A cell-permeable thiophenylethanone compound that acts a direct, reversible, and selective inhibitor of deubiquitylating enzymes (DUBs) USP7 and USP47 (IC50 = 8.01 & 8.74 µ,M, respectively). Exhibits only a minimal effect on other DUBs and proteases (>25 µ,M). Also shown to block UCH-L5 activity in HEK293T cell extracts, but not in intact cells. Stabilizes p53, HDM2, and p21 levels in HEK293T and HCT-116 cells and induces growth arrest (50% cytotoxicity concentration, CC50 = 16.6 and 7.83 µ,M).Note: A pan-DUB selective inhibitor PR-619 (Cat. No. 662141) is also available., A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50 = 8.01 & 8.74 µ,M, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 (Cat. No. 662141) targets (IC50 >50 µ,M). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 µ,M, 0.5 to 20 h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains.