RA-9
目录号: PL03607 纯度: ≥98%
CAS No. :919091-63-7
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中文名称
RA-9
中文别名
(3E,5E)-3,5-双(4-硝基亚苄基)哌啶-4-酮;化合物RA-9
英文名称
RA-9
英文别名
4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-, (3E,3E)-;(3E,5E)-3,5-Bis[(4-Nitrophenyl)methylene]-4-piperidinone;4-Piperidinone, 3,5-bis[(4-nitrophenyl)methylene]-, (3E,5E)-;RA-9 UPS inhibitor;RA-9;(3E,5E)-3,5-Bis[(4-nitrophenyl)methylene]-4-piperidinone (ACI)
Cas No.
919091-63-7
分子式
C19H15N3O5
分子量
365.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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.
性状
Solid
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C)配制储备液
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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