1. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Ferroptosis Glutathione Peroxidase Reactive Oxygen Species (ROS)
  3. Ferroptosis inducer-8

Ferroptosis inducer-8 是一种铁死亡 (ferroptosis) 诱导剂,对其他细胞死亡机制具有高选择性。Ferroptosis inducer-8 通过影响 ACSL4GPX4FTH1 来诱导铁死亡,从而破坏细胞内铁稳态和 GSH/GPX4 抗氧化防御系统,最终导致脂质过氧化积累。Ferroptosis inducer-8 也能诱导 ROS 的产生。Ferroptosis inducer-8 可抑制肿瘤生长,可用于三阴性乳腺癌 (TNBC) 的研究。

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Ferroptosis inducer-8

Ferroptosis inducer-8 Chemical Structure

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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 inducer-8 is a ferroptosis inducer with high selectivity for other cell death mechanism. Ferroptosis inducer-8 induces ferroptosis by affecting ACSL4, GPX4, and FTH1, thereby disrupting intracellular iron homeostasis and the GSH/GPX4 antioxidant defense system, ultimately leading to the accumulation of lipid peroxidation. Ferroptosis inducer-8 also induces ROS production. Ferroptosis inducer-8 inhibits tumor growth and can be used for research of triple-negative breast cancer (TNBC)[1].

体外研究
(In Vitro)

Ferroptosis inducer-8 与 GPX4 结合,降低 GPX4 的热稳定性[1]
Ferroptosis inducer-8 (Compound B23) (48 h) 在肿瘤细胞中表现出细胞毒性,IC50 分别为 0.08 μM (MCF-7)、0.04 μM (MDA-MB-231)、0.04 μM (MDA-MB-468)。 0.05 μM (HT29)、2.81 μM (A549)、0.06 μM (MPC-3) 和 2.23 μM (正常细胞 (MCF-10A))[1]
Ferroptosis inducer-8 (1 μM,48 小时) 选择性诱导 MDA-MB-231 和 MDA-MB-468 细胞的铁死亡,而不是其他细胞死亡机制,例如凋亡、坏死或自噬[1]
Ferroptosis inducer-8 (20-60 nM,7 小时) 在 MDA-MB-231 中诱导铁代谢紊乱,加剧脂质过氧化,并诱导活性氧 (ROS) 生成 (10 小时)。细胞[1]
Ferroptosis inducer-8 (20-60 nM,8 小时) 可上调 MDA-MB-231 细胞中 ACSL4 的表达,并下调 FTH1 和 GPX4 的表达[1]

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

Cell Viability Assay[1]

Cell Line: MDA-MB-231 and MDA-MB-468 cells
Concentration: 1 μM, co-incubation with Z-VAD-FMK (10 μM), Necrostatin-1 (10 μM) or 3-MA (5 mM); co-incubation with the ferroptosis inhibitors Fer-1 ( 1 μM), DFO (200 μM)), GSH (5 mM) or NAC (5 mM)
Incubation Time: Pretreated with various cell death inhibitors for 30 min, then co-incubation for 48 h
Result: Inhibited cell viability and the effect was rescued by Fer-1 ( HY-100579), Deferoxamine (DFO) (HY-B1625)), GSH (HY-D0187) or NAC (HY-B0215).
The cytotoxicity could not rescued by Z-VAD-FMK (HY-16658B), Necrostatin-1 (HY-15760), 3-MA (HY-19312).

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 20, 40, 60 nM
Incubation Time: 8 h
Result: Upregulated expression of ACSL4, downregulates FTH1 and GPX4 in MDA-MB-231 cells, and the modulatory effects were partially restored by Fer-1 (1 μM).
体内研究
(In Vivo)

Ferroptosis inducer-8 (1-4 mg/kg,静脉注射,每日一次,持续 21 天) 在异种移植模型中显示出抗肿瘤功效[1]

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

Animal Model: MDA-MB-231 xenograft model established in BALB/C nude mice (4 weeks)[1]
Dosage: 1, 2, 4 mg/kg
Administration: Daily tail vein injection (i.v.), at the corresponding doses for 21 days.
Result: Inhibited tumor growth in a concentration-dependent manner, with the tumor growth inhibition (TGI) rate of 78.46% (4 mg/kg), which was significantly higher than that in the positive control group (4 mg/kg RSL3 (HY-100218A), TGI = 27.21%).
Had lower toxicity (higher body weight) than RSL3 at high doses.
Showed no apparent toxicity to the hearts, livers, spleens, lungs or kidneys (H&E staining).
分子量

486.34

Formula

C22H25Cl2NO7

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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产品名称:
Ferroptosis inducer-8
目录号:
HY-174345
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