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RA-9
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
RA-9图片
CAS NO:919091-63-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
RA-9 是一种高效选择性蛋白酶体相关 DUBs 抑制剂，具有良好的毒性和抗癌活性。RA-9 阻断泛素依赖性蛋白降解而不影响 20S 蛋白酶体蛋白水解活性。RA-9 选择性诱导卵巢癌细胞株和供体原代培养细胞凋亡。RA-9 诱导卵巢癌细胞内质网应激反应。
Cas No.919091-63-7
别名(3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮
Canonical SMILESO=C1/C(CNC/C1=C\C2=CC=C([N+]([O-])=O)C=C2)=C/C3=CC=C([N+]([O-])=O)C=C3
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℃)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.