中文名：Elesclomol (STA-4783)
英文名：Elesclomol (STA-4783)
英文別名：N1',N3'-dimethyl-N1',N3'-di(phenylcarbonothioyl)malonohydrazide
純度：10mM in DMSO
貨號(hào)：E408561
包裝：1ml
Cas號(hào)：488832-69-5
存儲(chǔ)溫度：-80℃儲(chǔ)存
產(chǎn)品介紹：
Information
Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
In?vitro
Elesclomol significantly induces the expression of heat shock stress response genes and metallothionein genes, a signature transcription profile indicative of oxidative stress in Hs294T cells. Elesclomol (100 nM) rapidly induces Hsp70 RNA levels with a 4.8-fold increase at 1 hour and a 160-fold increase at 6 hours in Ramos Burkitt\'s lymphoma B cells in consistent with the intracellular ROS content which increases by 20% as early as 0.5 hour and 385% at 6 hours, and the induction of Hsp70 can be blocked by antioxidants N-acetylcysteine (NAC) and Tiron pretreatment. Elesclomol increases the number of early and late apoptotic cells with 3.7- and 11-fold through the induction of oxidative stress, which can be completely blocked by NAC, while having little effect on normal cells. Elesclomol significantly inhibits the cell viability of SK-MEL-5, MCF-7, and HL-60 with IC50 of 110 nM, 24 nM and 9 nM, respectively. Elesclomol induces copper-dependent ROS generation and cytoxicity in yeast. Instead of working through a specific cellular protein target, Elesclomol interacts with the electron transport chain (ETC), a biologically coherent set of processes occurring in the mitochondrion, to generate high levels of ROS within the organelle and consequently cell death.
In?vivo
Although Elesclomol (25-100 mg/kg) as a single agent shows no antitumor activity in nude mouse xenograft models of human breast cancers (MDA435, MCF7 and ZR-75-1), lung cancer (RER) or lymphoma (U937), Elesclomol substantially enhances the efficacy of chemotherapeutic agents such as paclitaxel in these models, both in terms of tumor regression and extended survival of mice.
Cell?Data
cell?lines：
Concentrations：Dissolved in DMSO at a concentration of 10 mM, final concentrations ~500 nM
Incubation?Time：18, or 24 hours
Powder?Purity:≥99%
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對(duì)應(yīng)頁(yè)面：https://www.aladdin-e.com/zh_cn/E408561.html
關(guān)鍵字： N1',N3'-dimethyl-N1',N3'-di(phenylcarbonothioyl)malonohydrazide
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代碼：688179），專注于科研試劑的研發(fā)、生產(chǎn)和銷售，已陸續(xù)建立多個(gè)工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅(jiān)持質(zhì)量第一，連續(xù)13年被評(píng)為“最受歡迎試劑品牌”。
阿拉丁目前常備庫(kù)存試劑產(chǎn)品品種超過(guò)7萬(wàn)種，SKU總數(shù)超過(guò)46萬(wàn)，產(chǎn)品線涵蓋了化學(xué)試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個(gè)領(lǐng)域，是國(guó)內(nèi)少數(shù)化學(xué)試劑到生物試劑全面發(fā)展的國(guó)產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國(guó)內(nèi)外電商平臺(tái)。