化合物RA-9 T8464

Product Introduction
Bioactivity


英文名: RA-9

描述: RA-9 是一种高选择性蛋白酶体相关的 DUBs 抑制剂，具有良好的毒性和抗癌活性。它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。它诱导卵巢癌细胞内质网应激反应，选择性诱导卵巢癌细胞株和供体原代培养细胞凋亡。

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4 mg/mL (10.95 mM)


关键字: Unfolded | cancer | RA 9 | DUBs | Inhibitor | Apoptosis | Response | Deubiquitinase | cells | inhibit | Protein | RA9 | ovarian | survival | RA-9

相关产品: ISRIB (trans-isomer) | Eragidomide | KRIBB11 | Psoralen | Valepotriate | VTP50469 | Amuvatinib | Diethyl phthalate | Thapsigargin | SZL P1-41

相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | DNA Damage & Repair Compound Library | Apoptosis Compound Library | Bioactive Compound Library

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