Cayman P22077

P22077 is a dual inhibitor of the deubiquitylating enzymes ubiquitin-specific protease 7 (USP7) and USP47 (EC₅₀s = 8.01 and 8.74 µM, respectively, in a fluorescence-based enzyme assay). It is selective for USP7 and USP47 over other USPs and proteases with EC₅₀ values greater than 50 µM. P22077 (25 µM) induces the accumulation of polyubiquitinated proteins in HEK293 cells. In neuroblastoma cells in vitro, P22077 blocks deubiquitylation of HDM2, a protein that normally deubiquitinates the tumor suppressor p53 leading to its degradation. When used at concentrations of 10 and 20 µM, it amplifies the cytotoxicity and p53-mediated apoptosis of doxorubicin (Item No. ) and etoposide (Item No. ) in neuroblastoma cells. P22077 inhibits tumor growth in neuroblastoma mouse xenograft models when administered at a dose of 20 mg/kg per day.

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