| 产品描述： | RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. |
| 靶点： |
IC50: 0.15 μM (HeLa cell);Proteasome |
| 体外研究： |
RA190 covalently binds to cysteine 88 of ubiquitin receptor RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins. Multiple myeloma (MM) lines, even those resistant to bortezomib, are sensitive to RA190 via endoplasmic reticulum stress-related apoptosis. RA190 stabilizes targets of human papillomavirus (HPV) E6 oncoprotein, and preferentially kills HPV-transformed cells |
| 体内研究： |
RA190 distributes to plasma and major organs excepting brain, and inhibits proteasome function in skin and muscle. RA190 administration profoundly reduces growth of multiple myeloma and ovarian cancer xenografts, and oral RA190 treatment retards HPV16+ syngeneic mouse tumor growth, without impacting spontaneous HPV-specific CD8+ T cell responses |
| 参考文献： |
1. Anchoori RK, et al. A bis-benzylidine piperidone targeting proteasome ubiquitin receptor RPN13/ADRM1 as a therapy for cancer. Cancer Cell. 2013 Dec 9;24(6):791-805. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.676 ml |
8.379 ml |
16.757 ml |
| 5 mM |
0.335 ml |
1.676 ml |
3.351 ml |
| 10 mM |
0.168 ml |
0.838 ml |
1.676 ml |
| 50 mM |
0.034 ml |
0.168 ml |
0.335 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