RA-9

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Chemical Structure| 919091-63-7 同义名 : -
CAS号 : 919091-63-7
货号 : A1280876
分子式 : C19H15N3O5
纯度 : 98%+
分子量 : 365.34
MDL号 : MFCD28400615
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(8.21 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.69mL

2.74mL

1.37mL

27.37mL

5.47mL

2.74mL
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