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CAS No.: 919091-63-7

RA-9 Catalog No. CSN26164

Synonyms: RA-9 UPS inhibitor

RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS) that targets deubiquitinating enzymes (DUB) without affecting 20S proteasome catalytic-core activity. Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors。

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The aberrant activity of deubiquitinating enzymes (DUBs) is linked to carcinogenesis and chemoresistance. RA-9 is a potent, cell-permeable inhibitor of 19S regulatory particle (RP)-associated DUBs. It blocks ubiquitin-dependent protein degradation without affecting the activity of 20S proteasome. Treatment of ES-2 cells with RA-9 (5 - 40 μM) resulted in a concentration-dependent accumulation of poly-ubiquitinated proteins in cells. RA-9 treatment (0.05 - 50 μM, 100 - 300s) dose- and time-dependently reduced the activity of 19S RP-associated DUB in ES-2 cells. The exposure of cisplatin-sensitive ovarian cancer cell lines TOV-21G and ES-2 with increasing concentrations of RA-9 (10 - 30 μM) for 48 hours decreased cell viability in a dose-dependent fashion. RA-9 exposure (1.25 μM and 5 μM) for 18 hours also led to a concentration-dependent increase in the fraction of G2-M cell cycle phase in ES-2 cells. Treatment of ES-2 cell lysates with 5 μM RA-9 for 24 hours resulted in time-dependent accumulation of the cleaved formed of PARP staring at 8-hour post-treatment. In NCr nu/nu mice inoculated with ES-2 ovarian cancer cells, a significant reduction in tumor burden was observed in the group treated with RA-9 (i.p., 5 mg/kg, one-day on, two-day off schedule) compared to the controls by day 5 of treatment^[1].
参考文献

[1] Coughlin K, Anchoori R, Iizuka Y, Meints J, MacNeill L, Vogel RI, Orlowski RZ, Lee MK, Roden RB, Bazzaro M. 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 Jun 15;20(12):3174-86. doi: 10.1158/1078-0432.CCR-13-2658

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7372 mL
- 13.6859 mL
- 27.3718 mL
- 5 mM
- 0.5474 mL
- 2.7372 mL
- 5.4744 mL
- 10 mM
- 0.2737 mL
- 1.3686 mL
- 2.7372 mL

技术信息

CAS号

919091-63-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H15N3O5

运输

蓝冰

分子量

365.34

别名

RA-9 UPS inhibitor

溶解度

DMSO	8.0 mg/mL (21.9 mM)
Water	Insoluble
Ethanol	Insoluble

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RA-9 Catalog No. CSN26164

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