首页 DNA Damage/DNA Repair Deubiquitinase RA-9
RA-9
编号 T8464    
CAS 919091-63-7     分子式 C19H15N3O5     分子量 365.34
靶点: Apoptosis;deubiquitinating enzymes (DUBs);
RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
选择批次  
规格 库存 单价 数量
2 mg 上海现货 344.00
5 mg 上海现货 492.00
10 mg 上海现货 738.00
25 mg 上海现货 1328.00
50 mg 上海现货 1992.00
100 mg 上海现货 2988.00
1 mL * 10 mM (in DMSO) 上海现货 582.00
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生物活性

产品描述

RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.

靶点活性

Apoptosis;deubiquitinating enzymes (DUBs),

体外活性

The characterization of RA-9 as a small-molecule inhibitor of proteasome-associated DUBs. Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. Loss of cell viability following RA-9 exposure is associated with an unfolded protein response as mechanism to compensate for unsustainable levels of proteotoxic stress.

体内活性

In vivo treatment with RA-9 retards tumor growth, increases overall survival, and was well tolerated by the host.

动物实验

Mice were inoculated i.p. with 100,000 ES-2 cells (in 100 μl DMEM) stably expressing GFP. When tumor was detectable (approx. 6 days post inoculation), mice were randomly assigned into two groups receiving RA-9 or 0.9% saline. Treatment with RA-9 was given i.p. on a one-day on, two-days off schedule. The control group received the vehicle alone at the same schedule. Working concentrations of RA-9 (10 mg/ml) were reached by dissolution in Cremophor EL and polyethylene glycol 400 (Sigma). Prior to each injection RA-9 was further diluted in 0.9% saline (working concentration 1mg/ml). To monitor for tumor growth, RA-9 treated and control mice were imaged with an IVIS SpectrumCT Pre-clinical in vivo imaging system (PerkinElmer) every other day. Animals were sacrificed when abdomens became distended to twice normal size.

化学信息

分子量

365.34

分子式

C19H15N3O5

CAS

919091-63-7

溶解度

DMSO: 4 mg/mL (10.95 mM), ultrasonic and warming and heat to 80°C

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.737 ml 13.686 ml 27.372 ml
5 mM 0.547 ml 2.737 ml 5.474 ml
10 mM 0.274 ml 1.369 ml 2.737 ml
50 mM 0.055 ml 0.274 ml 0.547 ml
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