目录号: HY-13865
Cell Cycle/DNA Damage-
P22077是泛素特异性蛋白酶（USP）7抑制剂，EC50为8.6 uM，还能抑制USP47。
Deubiquitinase
相关产品
BAY 11-7082-DUBs-IN-2-VLX1570-WP1130-b-AP15-HBX 19818-USP7/USP47 inhibitor-P005091-ML-323-SJB3-019A-LDN-57444-PR-619-SJB2-043-ML364-DUBs-IN-1-
生物活性
Description
P22077 is a potent inhibitor of ubiquitin-specific protease (USP) 7 (EC50=8.6 uM), P22077 also inhibits the closely related deubiquitinase (DUB) USP47.IC50 Value: 8.6 uM (EC50) [1]Target: USP7; USP47in vitro: 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 stabilized p53 by inducing HDM2 protein degradation in NB cells. 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 [2].in vivo: In an in vivo orthotopic NB mouse model, P22077 significantly inhibited the xenograft growth of three NB cell lines [2].
References
[1].Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12.
[2].Fan YH, et al. USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis. Cell Death Dis. 2013 Oct 17;4:e867.