产品详情
简单介绍：
I-BET762(GSK525762),BETInhibitor
详情介绍：
Product Information
| Molecular Weight: | 423.90 |
| Formula: | C22H22ClN5O2 |
| Purity: | ≥98% |
| CAS#: | 1260907-17-2 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
I-BET762 (GSK525762) is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~35 nM. It suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation. It is highly selective over other bromodomain-containing proteins. In vivo studies using I-BET762 have demonstrated efficacy in a range of oncology and immunoinflammatory models. I-BET762 is currently in clinical development for oncology indication.
How to Use:
- In vitro: I-BET762 was used at 0.5-1 µM final concentration in various in vitro assays.
- In vivo: I-BET762 could be dosed to the mice by oral administration at 10-30 mg/kg once per day.
Reference:
- 1. Mirguet O, et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. (2013) J Med Chem. 56(19):7501-15.
- 2. Zhao Y, et al. The making of I-BET762, a BET bromodomain inhibitor now in clinical development. (2013) J Med Chem. 56(19):7498-500.
Products are for research use only. Not for human use.
相关文章
