|Solubility:||DMSO up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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
- 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.
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