RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cell
RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
[1] Ravi K Anchoori, et al. Cancer Cell. 2013 Dec 9;24(6):791-805. [2] Y Song, et al. Leukemia. 2016 Sep;30(9):1877-86.
Cell experiment: | RA190 is dissolved in DMSO and diluted with cell culture medium. HeLa cells are treated with RA190 (0.2, 0.4, 0.6, 0.8, 1, 2, 3, 4, 5 μM) for 48 hr. Cell viability is assayed using commerical kit[1]. |
Animal experiment: | Mice: Mice are divided into two groups and treated daily i.p. with RA190 (10 mg/kg) or vehicle, and imaged again on day 7 and day 14. NOG mice (5 per group) are inoculated with 1X106 NCI-H929-GFP-Luc cells i.v., and after 4 weeks, mice are imaged for their luciferase activity and divided into two groups. Mice are treated i.p. with RA190 (20 mg/kg) or vehicle, and imaged again at the end of the treatment for their luciferase activity[1]. |
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. | |
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