产品号 #100-0544_C
胱氨酸转运蛋白抑制剂；诱发ferroptosis
概述
Erastin是一种胱氨酸转运蛋白抑制剂，在体外诱导铁致细胞死亡（Li等）。通过阻断Xc -系统，它诱导铁依赖性程序性细胞死亡，在癌症、神经系统疾病和急性肾损伤中发挥重要的调节作用（Li等）。在癌蛋白存在的情况下，它的活性增加（Dolma等人）。
癌症研究
·诱导表达Ras、SV40小T癌蛋白的细胞死亡（IC50 = 1.25 ~ 5 μg/mL）；Dolma等人)。
·通过谷氨酸释放试验（IC50 = 0.20 μM）测定，通过胱氨酸-谷氨酸反转运蛋白（系统Xc−）抑制胱氨酸摄取；Larraufie等人)。
Cell Type
Cancer Cells and Cell Lines
Area of Interest
Cancer
CAS Number
571203-78-6
Chemical Formula
C30H31ClN4O4
Molecular Weight
547.1 g/mol
Purity
≥ 98%
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
Resources and Publications
Educational Materials (3)
Publications (3)
Ferroptosis: past, present and future. Cell death {\&} disease 2020 feb
Abstract
Ferroptosis is a new type of cell death that was discovered in recent years and is usually accompanied by a large amount of iron accumulation and lipid peroxidation during the cell death process; the occurrence of ferroptosis is iron-dependent. Ferroptosis-inducing factors can directly or indirectly affect glutathione peroxidase through different pathways, resulting in a decrease in antioxidant capacity and accumulation of lipid reactive oxygen species (ROS) in cells, ultimately leading to oxidative cell death. Recent studies have shown that ferroptosis is closely related to the pathophysiological processes of many diseases, such as tumors, nervous system diseases, ischemia-reperfusion injury, kidney injury, and blood diseases. How to intervene in the occurrence and development of related diseases by regulating cell ferroptosis has become a hotspot and focus of etiological research and treatment, but the functional changes and specific molecular mechanisms of ferroptosis still need to be further explored. This paper systematically summarizes the latest progress in ferroptosis research, with a focus on providing references for further understanding of its pathogenesis and for proposing new targets for the treatment of related diseases.
Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility. Bioorganic {\&} medicinal chemistry letters 2015 nov
Abstract
Introducing a reactive carbonyl to a scaffold that does not otherwise have an electrophilic functionality to create a reversible covalent inhibitor is a potentially useful strategy for enhancing compound potency. However, aldehydes are metabolically unstable, which precludes the use of this strategy for compounds to be tested in animal models or in human clinical studies. To overcome this limitation, we designed ketone-based functionalities capable of forming reversible covalent adducts, while displaying high metabolic stability, and imparting improved water solubility to their pendant scaffold. We tested this strategy on the ferroptosis inducer and experimental therapeutic erastin, and observed substantial increases in compound potency. In particular, a new carbonyl erastin analog, termed IKE, displayed improved potency, solubility and metabolic stability, thus representing an ideal candidate for future in vivo cancer therapeutic applications.
Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells. Cancer cell 2003 mar
Abstract
We used synthetic lethal high-throughput screening to interrogate 23,550 compounds for their ability to kill engineered tumorigenic cells but not their isogenic normal cell counterparts. We identified known and novel compounds with genotype-selective activity, including doxorubicin, daunorubicin, mitoxantrone, camptothecin, sangivamycin, echinomycin, bouvardin, NSC146109, and a novel compound that we named erastin. These compounds have increased activity in the presence of hTERT, the SV40 large and small T oncoproteins, the human papillomavirus type 16 (HPV) E6 and E7 oncoproteins, and oncogenic HRAS. We found that overexpressing hTERT and either E7 or LT increased expression of topoisomerase 2alpha and that overexpressing RAS(V12) and ST both increased expression of topoisomerase 1 and sensitized cells to a nonapoptotic cell death process initiated by erastin.
更多信息
| Molecular Weight | 547.1 g/mol |
|---|---|
| Cas Number | 571203-78-6 |
| Chemical Formula | C30H31ClN4O4 |
| Purity | ≥ 98% |
PRODUCTS ARE FOR RESEARCH USE ONLY AND NOT INTENDED FOR HUMAN OR ANIMAL DIAGNOSTIC OR THERAPEUTIC USES UNLESS OTHERWISE STATED. FOR ADDITIONAL INFORMATION ON QUALITY AT STEMCELL, REFER TO WWW.STEMCELL.COM/COMPLIANCE.
