Elesclomol (STA-4783)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Elesclomol（STA-4783），最初是在用于促凋亡活性鉴定的基于细胞的表型筛选中获得的，是一种新型小分子，通过快速产生氧化应激（ROS）和诱导难以应对的氧化应激水平，从而有效诱导癌细胞凋亡。在人类肿瘤异种移植模型中，elesclomol对广谱类型的癌细胞均具有抗肿瘤活性，通过产生过量的ROS和升高氧化应激水平，从而导致癌细胞死亡。Elesclomol目前正作为一种新的癌症治疗方法用于研究，已证明，elesclomol具有延长研究对象中无进展生存期的能力。
参考文献：
Ronald K. Blackman, Kahlin Cheung-Ong, Marinella Gebbia, David A. Proia, Suqin He, Jane Kepros, Aurelie Jonneaux, Philippe Marchetti, Jerome Kluza, Patricia E. Rao, Yumiko Wada, Guri Giaever, Corey Nislow. Mitochondrial electron transport is the cellular target of the oncology drug elesclomol. PLoS ONE 2012; 7(1): e29798
Jessica R. Kirshner, Suqin He, Vishwasenani Balasubramanyam, Jane Kepros, Chin-Yu Yang, Mei Zhang, Zhenjian Du, James Barsoum, and John Bertin. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther 2008; 7:2319-2327
- 1. Albayrak G, Korkmaz FD, et al. "The outcomes of an impaired powerhouse in KRAS mutant lung adenocarcinoma cells by Elesclomol." J Cell Biochem. 2019 Jan 10. PMID:30628735
- 2. Li H, Guo S, et al."Lipopolysaccharide and heat stress impair the estradiol biosynthesis in granulosa cells via increase of HSP70 and inhibition of smad3 phosphorylation and nuclear translocation." Cell Signal. 2017 Jan;30:130-141. PMID:27940052
- 3. Ali A. Alshamrani, James L. et al. "Inhibiting Lactate Dehydrogenase A Enhances the Cytotoxicity of the Mitochondria Accumulating Antioxidant, Mitoquinone, in Melanoma Cells." Human Skin Cancer, Potential Biomarkers and Therapeutic Targets.October 19th 2016.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 400.5 |
| Cas No. | 488832-69-5 |
| Formula | C19H20N4O2S2 |
| Synonyms | STA 4783, STA4783 |
| Solubility | insoluble in H2O; ≥20.15 mg/mL in DMSO; ≥5.68 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 1-N',3-N'-bis(benzenecarbonothioyl)-1-N',3-N'-dimethylpropanedihydrazide |
| SDF | Download SDF |
| Canonical SMILES | CN(C(=S)C1=CC=CC=C1)NC(=O)CC(=O)NN(C)C(=S)C2=CC=CC=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
HSB2细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
200 nM；18小时 |
|
实验结果 |
在HSB2细胞中，Elesclomol增加早期和晚期凋亡细胞的数量（分别为3.7倍和11倍）。 |
| 动物实验 [2]: | |
|
动物模型 |
携带人乳腺癌（MDA435、MCF7和ZR-75-1）、肺癌 (RER) 或淋巴癌( U937) 的裸鼠模型 |
|
给药剂量 |
25 ~ 100 mg/kg；静脉注射 |
|
实验结果 |
在携带人乳腺癌（MDA435、MCF7和ZR-75-1）、肺癌 (RER) 或淋巴癌( U937) 的裸鼠模型中，单剂量Elesclomol (25 ~ 100 mg/kg) 没有抗癌活性。然而，Elesclomol显著增强化疗药物（如：紫杉醇）疗效，使肿瘤消退，并延长小鼠寿命。 |
|
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Jessica R. Kirshner, Suqin He, Vishwasenani Balasubramanyam, Jane Kepros, Chin-Yu Yang, Mei Zhang, Zhenjian Du, James Barsoum, and John Bertin. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol Cancer Ther 2008; 7:2319-2327 [2]. Gehrmann M. Drug evaluation: STA-4783--enhancing taxane efficacy by induction of Hsp70. Curr Opin Investig Drugs. 2006 Jun;7(6):574-80. |
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| 描述 | Elesclomol是一种新型有效的氧化应激诱导剂。 | |||||
| 靶点 | HSP70 | |||||
| IC50 | ||||||
化学结构
相关生物数据
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