| 货号 | 15022S |
| 供应商 | CST |
| 背景 | Carfilzomib, also known as PR-171, is a potent and irreversible epoxomycin-related proteasome inhibitor (1-4). It preferentially inhibits the chymotrypsin-like (CT-L) activity (low nanomolar IC50) of the 20S proteasome with greater than ten-fold selectivity over trypsin-like and caspase-like activities (1,2). CT-L inhibition with carfilzomib prevents degradation of short-lived misfolded and ubiquitinated proteins intended for proteasomal degradation, inducing cell cycle arrest and/or apoptosis in a variety of tumor cell lines (1-3). Carfilzomib has been shown to have greater antiproliferative activity against multiple myeloma (MM) cells than bortezomib and can overcome bortezomib-induced drug resistance (1). Synergistic interactions between carfilzomib and the histone deacetylase inhibitors vorinostat and entinostat have been observed (4). Proteasome inhibitors such as carfilzomib are important research tools for studying cellular degradation of the ubiquitin-proteasome pathway. |
| 存放说明 | -20C |
| 参考文献 | 1 . Kuhn, D.J. et al. (2007) Blood 110, 3281-90. 2 . Demo, S.D. et al. (2007) Cancer Res 67, 6383-91. 3 . Sacco, A. et al. (2011) Clin Cancer Res 17, 1753-64. 4 . Dasmahapatra, G. et al. (2011) Mol Cancer Ther 10, 1686-97. |
Chemical structure of carfilzomib. | |
Western blot analysis of extracts from NIH/3T3 cells, untreated (-) or treated with Carfilzomib (6 hr) at the indicated concentrations, using Ubiquitin Antibody #3933. | |
Western blot analysis of extracts from NIH/3T3 cells, untreated (-) or treated with Carfilzomib (6 hr) at the indicated concentrations, using p53 (1C12) Mouse mAb #2524 (upper) or β-Actin (13E5) Rabbit mAb #4970 (lower). |
