919091-63-7
中文名称
(3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮
英文名称
RA-9
CAS
919091-63-7
分子式
C19H15N3O5
分子量
365.34
MOL 文件
919091-63-7.mol
更新日期
2023/03/20 15:41:19
919091-63-7 结构式
基本信息
中文别名
化合物RA-9(3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮
英文别名
RA-9 UPS inhibitor4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-, (3E,5E)-
物理化学性质
熔点230-233 °C(Solv: ethyl ether (60-29-7); acetonitrile (75-05-8))
沸点588.5±50.0 °C(Predicted)
密度1.414±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C)
酸度系数(pKa)5.13±0.20(Predicted)
形态Solid
颜色Light yellow to yellow
(3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/09/19 | S0884 | (3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮 RA-9 | 919091-63-7 | 5mg | 794.58元 |
| 2025/09/19 | S0884 | (3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮 RA-9 | 919091-63-7 | 25mg | 2432.03元 |
常见问题列表
生物活性
RA-9 是一种具有细胞渗透性的蛋白酶体相关的 deubiquitinating enzymes (DUBs) 的强效选择性抑制剂，具有良好的毒性和抗癌活性。RA-9 可在卵巢癌细胞系中选择性地诱导凋亡。靶点
| Target | Value |
|
DUBs
() |
体外研究
RA-9 (10-30 μM; 48 hours) inhibits growth of ovarian cancer cell lines and primary cultures.
RA-9 (1.25-5 μM; 18 hours) causes cell cycle arrest and caspase-mediated apoptosis in ovarian cancer cells.
RA-9 (5 μM; 0-24 hours) induces ER-stress responses in ovarian cancer cells.
RA-9 (5 μM; over 24 hours) treatment results with time-dependent accumulation of the cleaved formed of PARP noticeable as early as 8 hours.
Cell Viability Assay
| Cell Line: | Cisplatin-sensitive ovarian cancer cell lines TOV-21G and ES-2, Cisplatin-resistant ovarian cancer cell lines HEY and OVCAR-3, primary ovarian cancer cells |
| Concentration: | 10, 20, 30 μM |
| Incubation Time: | 48 hours |
| Result: | Compromised the viability of ovarian cancer cells in a dose-dependent fashion. |
Cell Cycle Analysis
| Cell Line: | ES-2 cells |
| Concentration: | 1.25, 5 μM |
| Incubation Time: | 18 hours |
| Result: | Resulted in a dose-dependent increase in the fraction of ES-2 cells in the G2-M cell cycle phase. |
Western Blot Analysis
| Cell Line: | ES-2, SKOV-3 and TOV-21G ovarian cancer cells |
| Concentration: | 5 μM |
| Incubation Time: | 0-24 h |
| Result: | Caused a time-dependent increase in the steady levels of the early ER-stress marker GRP-78, as well as the late ER-stress markers IRE1-α and Ero1L-α. |
体内研究
RA-9 (5 mg/kg; i.p; one-day on, two-days off) inhibits human ovarian cancer cell growth in vivo and prolongs survival in a mouse model for ovarian cancer.
| Animal Model: | Six-week-old female immunodeficient (NCr nu/nu) mice |
| Dosage: | 5 mg/kg |
| Administration: | I.p; one-day on, two-days off |
| Result: | Significant reduction in tumor burden at day 12. |