| 产品描述： | RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines |
| 靶点： |
DUB; Apoptosis;Apoptosis; DUB |
| 体外研究： |
The characterization of RA-9 as a small-molecule inhibitor of proteasome-associated DUBs. Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. Loss of cell viability following RA-9 exposure is associated with an unfolded protein response as mechanism to compensate for unsustainable levels of proteotoxic stress. |
| 体内研究： |
In vivo treatment with RA-9 retards tumor growth, increases overall survival, and was well tolerated by the host. |
| 动物实验： |
Mice were inoculated i.p. with 100,000 ES-2 cells (in 100 μl DMEM) stably expressing GFP. When tumor was detectable (approx. 6 days post inoculation), mice were randomly assigned into two groups receiving RA-9 or 0.9% saline. Treatment with RA-9 was given i.p. on a one-day on, two-days off schedule. The control group received the vehicle alone at the same schedule. Working concentrations of RA-9 (10 mg/ml) were reached by dissolution in Cremophor EL and polyethylene glycol 400 (Sigma). Prior to each injection RA-9 was further diluted in 0.9% saline (working concentration 1mg/ml). To monitor for tumor growth, RA-9 treated and control mice were imaged with an IVIS SpectrumCT Pre-clinical in vivo imaging system (PerkinElmer) every other day. Animals were sacrificed when abdomens became distended to twice normal size. |
| 参考文献： |
1. Coughlin K, Anchoori R, Iizuka Y, et al. Small-molecule RA-9 inhibits proteasome-associated DUBs and ovarian cancer in vitro and in vivo via exacerbating unfolded protein responses. Clin Cancer Res. 2014;20(12):3174‐3186. doi:10.1158/1078-0432.CCR-13-2658 |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.739 ml |
13.695 ml |
27.39 ml |
| 5 mM |
0.548 ml |
2.739 ml |
5.478 ml |
| 10 mM |
0.274 ml |
1.369 ml |
2.739 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.548 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京