HBX41108,USP7Inhibitor

Biological Activity:

HBX41108 is a potent and selective ubiquitin-specific protease 7 (USP7) inhibitor with IC50 ~424 nM. Kinetics data indicate it is an uncompetitive reversible inhibition mechanism. It inhibits USP7-mediated p53 deubiquitination (IC50 ~0.8 μM). It can also stabilize p53 and activate the transcription of a p53 target gene without inducing genotoxic stress. HBX41108 inhibits cancer cell growth, and induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines.

How to Use:

In vitro: HBX41108 was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Colland F, et al. Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. (2009) Mol Cancer Ther. 8(8):2286-95.
• 2. Colombo M, et al. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. (2010) ChemMedChem. 5(4):552-8. 

产品留言

标题

联系人

联系电话

内容

验证码

点击换一张

注：1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!
2.如有必要,请您留下您的详细联系方式!