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Description: P22077 (P-22077; P 22077) is a potent, cell-permeable and selective inhibitor of ubiquitin-specific protease USP7 (ubiquitin-specific protease 7) with potential antitumor activity. It inhibits USP7 with an EC50 of 8.6 uM, and also inhibits the closely related USP47. P22077 potently induces apoptosis in NB cells with an intact USP7-HDM2-p53 axis but not in NB cells with mutant p53 or without human homolog of MDM2 (HDM2) expression. P22077 also significantly augmented the cytotoxic effects of doxorubicin (Dox) and etoposide (VP-16) in NB cells with an intact USP7-HDM2-p53 axis. Moreover, P22077 was found to be able to sensitize chemoresistant LA-N-6 NB cells to chemotherapy.
References: Assay Drug Dev Technol. 2011 Apr; 9(2):165-73; Chem Biol. 2011 Nov 23; 18(11):1401-12.
Chemical Name: 1-(5-((2, 4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
InChi Key: RMAMGGNACJHXHO-UHFFFAOYSA-N
InChi Code: InChI=1S/C12H7F2NO3S2/c1-6(16)11-5-9(15(17)18)12(20-11)19-10-3-2-7(13)4-8(10)14/h2-5H, 1H3
SMILES Code: CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O
P22077; P-22077; P 22077
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