HBX41108,USP7Inhibitor
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產品名稱: HBX41108,USP7Inhibitor
產品型號: M60244-2s
產品展商: 其它品牌
產品文檔: 無相關文檔
簡單介紹
HBX41108,USP7Inhibitor
HBX41108,USP7Inhibitor
的詳細介紹
Product Information
| Molecular Weight: |
266.64 |
| Formula: |
C13H3ClN4O
|
| Purity: |
≥98% |
| CAS#: |
924296-39-9 |
| Solubility: |
DMSO up to 100 mM |
| Chemical Name: |
(3E,5E)-1-acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one |
| Storage: |
Powder: 4oC 1 year.
DMSO: 4oC 3 month;
-20oC 1 year. |
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.?
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Products are for research use only. Not for human use.
