919091-63-7
中文名稱
(3E,5E)-3,5-雙(4-硝基亞芐基)哌啶-4-酮
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物RA-9(3E,5E)-3,5-雙(4-硝基亞芐基)哌啶-4-酮
英文別名
RA-9 UPS inhibitor4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-, (3E,5E)-
物理化學(xué)性質(zhì)
熔點(diǎn)230-233 °C(Solv: ethyl ether (60-29-7); acetonitrile (75-05-8))
沸點(diǎn)588.5±50.0 °C(Predicted)
密度1.414±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C)
酸度系數(shù)(pKa)5.13±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
(3E,5E)-3,5-雙(4-硝基亞芐基)哌啶-4-酮價(jià)格(試劑級(jí))
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | S0884 | (3E,5E)-3,5-雙(4-硝基亞芐基)哌啶-4-酮 RA-9 | 919091-63-7 | 5mg | 794.58元 |
| 2024/11/08 | S0884 | (3E,5E)-3,5-雙(4-硝基亞芐基)哌啶-4-酮 RA-9 | 919091-63-7 | 25mg | 2432.03元 |
常見(jiàn)問(wèn)題列表
生物活性
RA-9 是一種具有細(xì)胞滲透性的蛋白酶體相關(guān)的 deubiquitinating enzymes (DUBs) 的強(qiáng)效選擇性抑制劑，具有良好的毒性和抗癌活性。RA-9 可在卵巢癌細(xì)胞系中選擇性地誘導(dǎo)凋亡。靶點(diǎn)
| Target | Value |
|
DUBs
() |
體外研究
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. |
體內(nèi)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. |