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化學性質(zhì):
規(guī)格 | 10mM*1 mL in DMSO 5mg 10mg 50mg 100mg |
CAS | 919091-63-7 |
別名 | N/A |
化學名 | N/A |
分子式 | C19H15N3O5 |
分子量 | 365.34 |
溶解度 | DMSO: 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C) |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells[1].
RA-9 (10-30 μM; 48 hours) inhibits growth of ovarian cancer cell lines and primary cultures[1].RA-9 (1.25-5 μM; 18 hours) causes cell cycle arrest and caspase-mediated apoptosis in ovarian cancer cells[1].RA-9 (5 μM; 0-24 hours) induces ER-stress responses in ovarian cancer cells[1].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[1]. Cell Viability Assay[1] 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
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[1]. Animal Model: Six-week-old female immunodeficient (NCr nu/nu) mice[1]
[1]. Coughlin K, et al. Small-molecule RA-9 inhibits proteasome-associated DUBs and ovarian cancer in vitro and in vivo via exacerbating unfolded protein responses. Clin Cancer Res. 2014;20(12):3174-3186.
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原創(chuàng)作者:上海莼試生物技術有限公司
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