CEP-18770
| CAS号 | 847499-27-8 | 货号 | BCP05719 |
| 中文名 | CEP-18770 | ||
| 英文名 | CEP-18770 | ||
| 中文别名 | |||
| 英文别名 | Delanzomib;CEP18770;CEP 18770;CIP 18770;CT 47098;NPH 007098; | ||
| 分子式 | C21H28BN3O5 | 分子量 | 413.28 |
| 生物活性 | CEP-18770 demonstrates marginal prevention of the tryptic and peptidyl gultamyl activities of the protesome. The IC50 values of CEP-18770 are similar to those of bortezomib, with the chymotryptic and caspase-like activities being inhibited at low-nanomolar concentrations.CEP-18770 inhibits A2780 ovarian cancer cells, PC3 prostate cancer, H460, LoVo colon cancer, RPMI8226 multiple myeloma cancer and HS-Sultan anaplastic non-Hodgkin lymphoma with IC50 values of 13.7, 22.2, 34.2 11.3, 5.6 and 8.2 nM, respectively.CEP-18770 blocks the ubiquitin-proteasome pathway in several MM and in the chronic myelogenous leukemia cell line, K562. CEP-18770 causes an accumulation of ubiquitinated proteins over 4 to 8 hours with a profile similar to that observed after bortezomib treatment.IκBα degradation is completely blocked by pretreatment with CEP-18770. CEP-18770 significantly inhibits high levels of NF-κB activity in both RPMI-8226 and U266 cells. The time- and concentration-dependent suppression o | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | Proteasome | ||
结构式
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