1. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Ferroptosis Reactive Oxygen Species (ROS)
  3. Ferroptosis-IN-21

Ferroptosis-IN-21  (Synonyms: 1,2,3,4-Tetrahydroquinolin-8-ol; 8-hydroxy-1,2,3,4-tetrahydroquinoline)

目录号: HY-W002942
产品使用指南 技术支持

Ferroptosis-IN-21 是一种铁死亡 (ferroptosis) 抑制剂,通过直接清除过氧自由基以抑制铁死亡,从而对抗肾脏缺血再灌注损伤。Ferroptosis-IN-21 对肾小管上皮细胞中的多种铁死亡诱导剂均表现出纳摩尔级别的广谱抑制效力,并能强效抑制脂质活性氧 (ROS) 的积累。Ferroptosis-IN-21 可显著减轻小鼠肾脏缺血再灌注损伤,具体表现为组织学损伤和功能受损得到改善、炎症细胞因子表达下降,以及 4-羟基壬烯酸等脂质过氧化生物标志物减少。Ferroptosis-IN-12 可用于铁死亡靶向药物开发领域的研究。

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Ferroptosis-IN-21

Ferroptosis-IN-21 Chemical Structure

CAS No. : 6640-50-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ferroptosis-IN-21 is a ferroptosis inhibitor that protects against renal I/R injury by suppressing ferroptosis and directly scavenging peroxyl radicals. Ferroptosis-IN-21 displays broad-spectrum anti-ferroptotic efficacy across multiple inducers in renal tubular epithelial cells, with nanomolar potency and robust suppression of lipid Reactive Oxygen Species (ROS). Ferroptosis-IN-21 significantly ameliorates renal I/R injury in mice, reducing histological damage, functional impairment, and inflammatory cytokine expression, while decreasing lipid peroxidation biomarkers such as 4-hydroxynonenal. Ferroptosis-IN-12 can be used for research in the field of ferroptosis-targeted drug development[1].

体外研究
(In Vitro)

Ferroptosis-IN-21 (compound 6) (0.01-10 μM,24 小时) 在 HT-1080 细胞中表现出纳摩尔级细胞保护活性 (EC50 = 61.7 nM),于 200 nM 浓度下可完全逆转细胞死亡,并且能剂量依赖性地保护人肾皮质上皮细胞 (HKC) 和人肾近曲小管上皮细胞 (HK-2) 细胞免受 RSL-3 (HY-100218A) 与 FIN-56 诱导的铁死亡,进而证实了其广谱抗铁死亡功效[1]
Ferroptosis-IN-21 (50-500 nM,24 小时) 显著抑制 RSL-3 诱导的脂质 ROS 积累和 MDA 升高,且对 GPX4 蛋白水平无影响[1]
Ferroptosis-IN-21 (10 µM) 不具备铁离子螯合能力,从而排除了其通过铁螯合机制发挥作用的可能性[1]
Ferroptosis-IN-21 (1-80 µM,30 分钟) 在无细胞 DPPH 检测中表现出强大的直接自由基清除活性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HT-1080, HKC and HK-2 cells
Concentration: 0.01-10 μM
Incubation Time: 24 h
Result: Exhibited nanomolar cytoprotective activity with an EC50 of 61.7 nM in HT-1080 cells.
Completely reversed RSL3-induced cell death in HT-1080 cells at the dose of 200 nM.
Exhibited significant cytoprotective effects on both HKC and HK-2 cells under RSL3-induced ferroptosis, displaying a concentration-dependent relationship, with the EC50 values of 361 and 258 nM, respectively.
Effectively inhibited FIN56-induced cell death in both HKC and HK-2 cells.

Western Blot Analysis[1]

Cell Line: HKC cells
Concentration: 500 nM
Incubation Time: 24 h
Result: Did not significantly alter GPX4 protein expression in either untreated or RSL3- stimulated cells.
体内研究
(In Vivo)

Ferroptosis-IN-21 (5 和 10 mg/kg,腹腔注射,造模前24及1小时) 在肾脏缺血再灌注小鼠模型中展现出对缺血性急性肾损伤的强大的肾脏保护作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (8-12 weeks old) subjected to bilateral renal ischemia (40 min) and reperfusion (24 h) [1]
Dosage: 5 and 10 mg/kg
Administration: i.p., 24 hours and 1 hour pre-treatment
Result: Reduced the serum creatinine, blood urea nitrogen (BUN), and kidney coefficient relative to the I/R group.
Conferred substantial structural protection, with the 10 mg/kg dose yielding the most notable histological preservation.
Markedly suppressed mRNA expression levels of KIM-1 and NGAL in a dose-dependent manner.
Significantly reduced the expression of TNF-α, IL1-β, IL-6, and MCP-1 upregulated by I/R insult in a dose-dependent manner, indicating an anti-inflammatory effect.
Markedly reduced I/R-induced 4-HNE accumulation.
分子量

149.19

Formula

C9H11NO

CAS 号
中文名称

1,2,3,4-四氢-8-羟基喹啉

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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