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RSL3

Ferroptosis Activators
    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 1219810-16-8
  • 分子式: C23H21ClN2O5
  • 分子量: 440.88
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Compound libraries (12333)

基本描述

英文别名 (1S,3R)-RSL3 | 1H-​Pyrido[3,​4-​b]​indole-​3-​carboxylic acid, 2-​(2-​chloroacetyl)​-​2,​3,​4,​9-​tetrahydro-​1-​[4-​(methoxycarbonyl)​phenyl]​-​, methyl ester, (1S,​3R)​-
规格或纯度 10mM in DMSO
英文名称 RSL3
生化机理 RSL3 ((1S,3R)-RSL3)是一种不依赖于 VDAC 的铁氧化激活剂,对携带致癌 RAS 的肿瘤细胞具有选择性。RSL3 与 GPX4 结合,使 GPX4 失活,从而介导 GPX4 调节的铁变态反应。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍

RSL3 ((1S,3R)-RSL3) 是一种谷胱甘肽过氧化物酶 4 (GPX4) 的抑制剂 (ferroptosis 激动剂),可降低 GPX4 的表达,诱导头颈部癌细胞的肥大性死亡。在 HN3 耐受细胞中,可增加 p62 和 Nrf2 的蛋白水平,使 Keap1 灭活。

用途

1S,3R-RSL 3已用于:
研究其作为谷胱甘肽过氧化物酶4(GPX4)抑制剂,对脑室下区多形性胶质母细胞瘤(GBM)细胞死亡的影响
研究其作为GPX4抑制剂和铁死亡诱导剂对小鼠心肌细胞死亡和心功能衰竭的影响
在细胞活力检测中作为HT-1080细胞铁死亡诱导剂

Information

RSL3 RSL3 ((1S,3R)-RSL3) is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis.
In vitro

Ferroptosis-inducing compounds inactivate GPX4 by direct binding or by depleting glutathione.After binding to GPX4, RSL3 inactivates GPX4 to induce ROS production from lipid peroxidation. RSL3\'s ability to induce synthetic lethality with oncogenic RAS is rapid and quite potent. This compound inhibits the growth of BJ-TERT/LT/ST/RASV12 and DRD cells as low as 10 ng/mland started to kill sensitive cells as early as 8 hr after treatment.

In vivo

Prostaglandin-endoperoxide synthase (PTGS) is the key enzyme in prostaglandin biosynthesis. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2. PTGS2 encoding cyclooxygenase-2 (COX-2) is significantly upregulated after treatment with RSL3 and erastin in mice.
Cell Data

cell lines:MOLT-4 cell lines and Reh (pre-B cells)

Concentrations:1 µg/ml

Incubation Time:16hrs

Powder Purity:≥99%

关联靶点(人)

GPX4 Tchem 磷脂氢过氧化物谷胱甘肽过氧化物酶(Phospholipid hydroperoxide glutathione peroxidase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Isomeric SMILES COC(=O)[C@H]1CC2=C([C@@H](N1C(=O)CCl)C3=CC=C(C=C3)C(=O)OC)NC4=CC=CC=C24
PubChem CID 1750826
分子量 440.88

安全和危险性(GHS)

RIDADR NONHforallmodesoftransport

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

引用文献

1. Xiaosi Lin , Le Dong, Qing Miao, Zhaobin Huang, Fang Wang.  (2024)  Cycloheptylprodigiosin from marine bacterium Spartinivicinus ruber MCCC 1K03745T induces a novel form of cell death characterized by Golgi disruption and enhanced secretion of cathepsin D in non-small cell lung cancer cell lines.  European Journal of Pharmacology,  无  (974): (176608).  [PMID:38663542] [10.1016/j.ejphar.2024.176608]
2. Haoze Song, Jing Liang, Yuanyuan Guo, Yang Liu, Kuiru Sa, Guohong Yan, Wen Xu, Wei Xu, Lixia Chen, Hua Li.  (2024)  A potent GPX4 degrader to induce ferroptosis in HT1080 cells.  EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,  265  (116110).  [PMID:38194774] [10.1016/j.ejmech.2023.116110]
3. Zhao Hongting, Zhang Meng, Zhang Jinghua, Sun Zichen, Zhang Wenxin, Dong Weichen, Cheng Chen, Yao Yongzhong, Li Kuanyu.  (2023)  Hinokitiol-iron complex is a ferroptosis inducer to inhibit triple-negative breast tumor growth.  Cell and Bioscience,  13  (1): (1-15).  [PMID:37179385] [10.1186/s13578-023-01044-0]
4. Yu-Chen Chen, Qiong Zheng, Hui Lu, Yi-Xin Zhuang, Ting-Ting Gong, Lie-Feng Ma, Zha-Jun Zhan.  (2023)  Neuroprotective flavonoids from Epimedium brevicornu by inhibition of ferroptosis.  Phytochemistry Letters,  55  (80).  [10.1016/j.phytol.2023.04.003]
5. Fan Zhang, Hualong Zhen, Hengshun Cheng, Fengying Hu, Yunfei Jia, Binbin Huang, Minmin Jiang.  (2022)  Di-(2-ethylhexyl) phthalate exposure induces liver injury by promoting ferroptosis via downregulation of GPX4 in pregnant mice.  Frontiers in Cell and Developmental Biology,  10  (1014243).  [PMID:36438553] [10.3389/fcell.2022.1014243]

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