1. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Ferroptosis Glutathione Peroxidase Reactive Oxygen Species (ROS) Mitochondrial Metabolism
  3. Ferroptosis inducer-15

Ferroptosis inducer-15 是一种铁死亡 (ferroptosis) 诱导剂。Ferroptosis inducer-15 可下调 GPX4 的表达,通过活性氧 (ROS) 累积触发脂质过氧化,并破坏线粒体膜电位以诱导铁死亡。Ferroptosis inducer-15 可提高脾脏中 CD4+ T 细胞的比例,促进 CD8+ 细胞毒性 T 细胞向肿瘤组织浸润,并激活抗肿瘤免疫应答。Ferroptosis inducer-15 对结直肠癌细胞具有抗增殖活性,且在异种移植小鼠模型中可抑制肿瘤生长,同时无显著体重降低。Ferroptosis inducer-15 可用于癌症相关研究,例如结直肠癌研究。

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Ferroptosis inducer-15

Ferroptosis inducer-15 Chemical Structure

CAS No. : 3097756-33-4

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查看 Glutathione Peroxidase 亚型特异性产品:

  • 生物活性

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生物活性

Ferroptosis inducer-15 is a ferroptosis inducer. Ferroptosis inducer-15 downregulates GPX4 expression, triggers lipid peroxidation via ROS accumulation, and disrupts mitochondrial membrane potential to drive ferroptosis. Ferroptosis inducer-15 increases splenic CD4+ T cell proportion, promotes CD8+ cytotoxic T cell tumor infiltration, and activates antitumor immune responses. Ferroptosis inducer-15 exerts antiproliferative activity against colorectal cancer cells and inhibits tumor growth in xenograft mice models without significant body weight loss. Ferroptosis inducer-15 can be used for the research of cancer, such as colorectal cancer[1].

IC50 & Target[1]

GPX4

 

体外研究
(In Vitro)

Ferroptosis inducer-15 (Compound 5k) (48 h) 可强效抑制 HCT116 结直肠癌细胞的增殖,其 IC50 为 0.81 μM,且对 SW480、SW620、HT29、HepG2 及 MCF-7 细胞表现出不同程度的抗增殖活性 (IC50 = 2.43-21.84 μM)[1]
Ferroptosis inducer-15 对 HCT116 细胞的细胞毒性依赖于铁死亡,与铁死亡特异性抑制剂共处理后细胞死亡得到逆转的结果可证明这一点[1]
Ferroptosis inducer-15 (1 μM; 24 h) 可显著提高 HCT116 结直肠癌细胞内的 ROS、Fe2+ 和脂质过氧化水平[1]
Ferroptosis inducer-15 (1 μM; 24 h) 可破坏 HCT116 结直肠癌细胞的线粒体膜电位,并诱导铁死亡相关的线粒体形态学改变[1]
Ferroptosis inducer-15 (0.5-2 μM; 24 h) 可下调 HCT116 结直肠癌细胞中 SLC7A11、FTH1 和 GPX4 的表达,并上调 ACSL4 的表达,表明其通过 System Xc/GPX4 通路诱导铁死亡[1]
Ferroptosis inducer-15 (1 μM) 可直接与 HCT116 结直肠癌细胞中的 GPX4 蛋白结合,在温度升高条件下增强 GPX4 的稳定性 (40-60°C)[1]
Ferroptosis inducer-15 (0.5-2 μM) 以浓度依赖的方式降低 HCT116 结直肠癌细胞中 GPX4 的 mRNA 表达水平[1]

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

Immunofluorescence[1]

Cell Line: HCT116 (colorectal adenocarcinoma)
Concentration: 1 μM
Incubation Time: 24 h
Result: Increased the fluorescence intensity DCFH-DA.

Western Blot Analysis[1]

Cell Line: HCT116 (colorectal adenocarcinoma)
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Resulted in concentration-dependent downregulation of SLC7A11, FTH1, and GPX4 protein expression, and upregulation of ACSL4 protein expression in HCT116 cells.
体内研究
(In Vivo)

Ferroptosis inducer-15 (Compound 5k)(25-50 mg/kg,腹腔注射,每 2 天 1 次,共 13 天) 在 CT26 结直肠癌异种移植模型中表现出剂量依赖性的体内抗肿瘤活性,在 50 mg/kg 剂量下的肿瘤抑制率达 54.9%;同时该化合物可通过提高 CD4+ 和 CD8+ T 淋巴细胞比例激活抗肿瘤免疫,且无明显全身毒性[1]

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

Animal Model: BALB/c (5 weeks old, male/female, subcutaneous CT26 colon tumor cell implantation)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.p.; once every 2 days; 13 days
Result: Achieved a tumor inhibition rate of 42.5%.
Achieved a tumor inhibition rate of 54.9%.
Did not induce significant body weight loss or obvious pathological changes in heart, liver, spleen, lung, or kidney tissues.
Increased the proportion of CD4+ T lymphocytes in the spleen by 1.3% and CD8+ T lymphocytes by 2.6% (at 25 mg/kg).
Increased the proportion of CD4+ T lymphocytes in the spleen by 6.2% and CD8+ T lymphocytes by 7.2% (at 50 mg/kg).
分子量

666.62

Formula

C31H41NO10Se

CAS 号
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.

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参考文献
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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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Ferroptosis inducer-15
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