1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Ferroptosis Keap1-Nrf2 Glutathione Peroxidase Reactive Oxygen Species (ROS)
  3. Ferroptosis inducer-13

Ferroptosis inducer-13 是一种 5′- 异戊二烯基化的查尔酮衍生物,它通过改变 Nrf2/xCT/GPX4 通路活性,有效诱导人非小细胞肺癌 (NSCLC) 细胞发生铁死亡 (ferroptosis)。Ferroptosis inducer-13 在体外表现出强效的抗增殖作用,并在 NSCLC 小鼠模型中抑制肿瘤生长。Ferroptosis inducer-13 可用于 NSCLC 的研究。

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Ferroptosis inducer-13

Ferroptosis inducer-13 Chemical Structure

CAS No. : 3085517-19-4

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生物活性

Ferroptosis inducer-13 is a 5′-prenylated chalcone derivative that effectively induces ferroptosis in human non-small cell lung cancer (NSCLC) cells by altering the activity of the Nrf2/xCT/GPX4 pathway. Ferroptosis inducer-13 exhibits potent anti-proliferative effects in vitro, and inhibits tumour growth in a NSCLC mouse model. Ferroptosis inducer-13 can be used for NSCLC research[1].

IC50 & Target[1]

GPX4

 

体外研究
(In Vitro)

Ferroptosis inducer-13 (compound 4a) (72 小时) 对癌细胞表现出强效的广谱抗增殖活性,IC50 值分别为 2.11 μM (PC9)、2.17 μM (MDA-MB-231)、3.81 μM (SMMC-7721) 和 4.10 μM (SGC-7901)[1]
Ferroptosis inducer-13 (0-40 μM;24-72 小时) 以剂量依赖及时间依赖性的方式抑制 NSCLC 细胞 (PC9 和 H1975) 增殖[1]
Ferroptosis inducer-13 (20 μM;24 小时) 可诱导非小细胞肺癌细胞 (PC9 和 H1975) 发生铁死亡[1]
Ferroptosis inducer-13 (0-40 μM;24 小时) 导致 GSH 耗竭,增加 Fe2+ROS 和 LPO 水平,并通过调节 PC9 和 H1975 细胞中的 Nrf2/xCT/GPX4 信号通路诱导铁死亡[1]

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

Cell Viability Assay[1]

Cell Line: PC9, H1975
Concentration: 0, 2.5, 5, 10, 20, 40 μM
Incubation Time: 24, 48, 72 h
Result: Gradually decreased cell viability of PC9 and H1975 cells in a concentration manner.
Exhibited significant anti-proliferative effects on NSCLC cells (PC9 and H1975) in a time- and concentration-dependent manner.

Cell Viability Assay[1]

Cell Line: PC9, H1975
Concentration: 20 μM
Incubation Time: 12 h
Result: Significantly enhanced cell viability by approximately 20% when combined with ferroptosis inhibitor.

Immunofluorescence[1]

Cell Line: PC9, H1975
Concentration: 20 μM
Incubation Time: 24 h
Result: Moderately reversed the GPX expression when combined with ferroptosis inhibitor.

Western Blot Analysis[1]

Cell Line: PC9, H1975
Concentration: 0, 5, 10, 20, 40 μM
Incubation Time: 24 h
Result: Significantly decreased Nrf2 levels in both cytoplasmic and nuclear fractions while reducing xCT and GPX4 expression.
体内研究
(In Vivo)

Ferroptosis inducer-13 (2 和 5 mg/kg;腹腔注射;每 3 天一次,持续 18 天) 可抑制 PC9 异种移植小鼠模型中的肿瘤生长,且具有良好的安全性[1]

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

Animal Model: Female Balb/c nude mice (16-20 g) subcutaneously injected with PC9 cells[1]
Dosage: 2, 5 mg/kg
Administration: i.p.; every 3 days for 18 days
Result: Exhibited tumor growth suppression with minimal impact on body weight.
Caused no significant organ toxicity in mice.
Significantly downregulated the protein expression of xCT and GPX4 in tumor tissues compared with the control group.
分子量

337.41

Formula

C21H23NO3

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-13
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