2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Cell Cycle/DNA Damage
  3. Glutathione Peroxidase Ferroptosis Lipoxygenase Reactive Oxygen Species (ROS) DNA/RNA Synthesis
  4. GPX4-IN-19

GPX4-IN-19 是一种有效的 GPX4 抑制剂 (IC50 = 0.311 μM)，与 GPX4 的 Sec 46 位点共价结合。GPX4-IN-19 具有很强的抗增殖活性和铁死亡 (ferroptosis) 高选择性。GPX4-IN-19 可导致细胞内 Fe²⁺ 积累，进而导致脂质过氧化物 (LPOs) 和活性氧 (ROS) 水平升高，最终诱导铁死亡 (ferroptosis) 并造成 DNA 损伤。GPX4-IN-19 可用于三阴性乳腺癌 (TNBC) 的研究。

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GPX4-IN-19

GPX4-IN-19 Chemical Structure

CAS No. : 3102894-57-2

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GPX4-IN-19 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GPX4-IN-19 is an effective GPX4 inhibitor (IC50 = 0.311 μM), covalently binds to the Sec 46 site of GPX4. GPX4-IN-19 shows strong anti-proliferative activity with high ferroptosis selectivity. GPX4-IN-19 causes intracellular Fe²⁺ accumulation, leading to increased levels of lipid peroxides (LPOs) and reactive oxygen species (ROS), which induces ferroptosis and subsequently results in DNA damage. GPX4-IN-19 can be used for the study of Triple-Negative Breast Cancer (TNBC)[1].

体外研究
(In Vitro)

GPX4-IN-19 (Compound Y19) (72 小时) 对六种癌细胞系 (MCF-7、MDA-MB-231、PC-3、MDA-MB-468、PANC-1 和 ASPC-1) 表现出有效的抗增殖活性 (IC50：0.021-0.094 μM)[1]。
GPX4-IN-19 (12.5-50 nM，2 周) 可有效抑制细胞增殖，而添加抑制剂 Ferrostatin-1 (HY-100579) (Fer-1) 可逆转 MDA-MB-231 细胞的增殖抑制作用。
GPX4-IN-19 (50 nM，8 小时) 可导致 MDA-MB-231 细胞线粒体出现典型的形态学变化，例如线粒体外膜破裂、线粒体体积缩小以及线粒体内膜嵴减少或消失。
GPX4-IN-19 (12.5-50 nM，8 小时) 可剂量依赖性地增加 MDA-MB-231 细胞内 Fe²⁺ 浓度、脂质过氧化物 (LPO) 积累、丙二醛 (MDA) 含量和活性氧 (ROS) 水平。
GPX4-IN-19 (12.5-50 nM，8 小时) 通过增加 γH2AX 的表达导致 MDA-MB-231 细胞 DNA 损伤，而这种 DNA 损伤可被 Fer-1 等抑制剂显著减弱。
GPX4-IN-19 (1 μM，2 小时) 可降低 MDA-MB-231 细胞中 GPX4 蛋白在相同温度下的降解温度，表明 GPX4-IN-19 降低了 GPX4 蛋白的热稳定性。
GPX4-IN-19 (12.5-nM，8 小时) 在对 GPX4 抑制剂 RSL3 或 ML162 耐药的 MDA-MB-231 细胞系变体 (MDA-MB-231-RSL3 和 MDA-MB-231-ML162) 中表现出显著的耐药性。
GPX4-IN-19 (12.5-50 nM，4-12 小时) 以浓度依赖的方式降低 MDA-MB-231 细胞中的 GPX4 水平。根据时间分析，GPX4 表达在 4 小时开始升高，此时 xCT 水平变化甚微；但随后在 8 小时 GPX4 表达下降，同时 xCT 表达显著升高。

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

GPX4-IN-19 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 2 weeks
Result: Effectively inhibited cell proliferation, and the addition of the inhibitor Fer-1 reversed the inhibition of cell proliferation in MDA-MB-231 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 8 h
Result: Increased expression of DNA damage marker γH2AX.
Decreased the level of GPX4 in a concentration-dependent manner.
Didn't inhibit other proteins contained selenium, including Glutathione peroxidase 1 (GPX1) and Thioredoxin reductase 1 (TXNRD1).
FTH1 was significantly decreased with the concentration change.
Increased ACSL4 expression levels.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 8 h
Result: Reduced GPX4 level in a concentration-dependent manner in MDA-MB-231 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 12.5 nM, 25 nM, 50 nM
Incubation Time: 4 h, 8 h, 12 h
Result: The expression of GPX4 increased at 4 h, and the xCT level of the upstream signaling pathway hardly changed at this time, but the expression level of GPX4 decreased and the expression level of xCT increased at 8h.
体内研究
(In Vivo)

GPX4-IN-19 (5 mg/kg，10 mg/kg，腹腔注射，每两天一次，持续 24 天) 在 MDA-MB-231 荷瘤小鼠模型中表现出剂量依赖性的抗肿瘤作用，且不引起明显的体重减轻、血液生化指标异常或器官病理损伤，显示出良好的安全性[1]。

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

Animal Model: MDA-MB-231 cells (1 × 107 cells in 200 μL suspension, mixed 1:1 with Matrigel and PBS) are subcutaneously injected into the left flank of female BALB/c nude mice (4 to 5weeks old)[1].
Dosage: 5 mg/kg, 10 mg/kg
Administration: I.p., every two days for 24 days
Result: Tumor growth was inhibited in a dose-dependent manner, tumor growth inhibition (TGI) of 72.53 % at 10 mg/kg.
Ki67-positive tumor cells were decreased.
GPX4 was significantly decreased compared with the control group.
Revealed no apparent morphological abnormalities in major organs, including the heart, liver, spleen, lungs, and kidneys.
Could not destroy the function of the liver, the kidneys, and the heart.
分子量

395.81

Formula

C19H19ClFNO5
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.
纯度 & 产品资料
参考文献

GPX4-IN-19 相关分类

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Keywords:

GPX4-IN-193102894-57-2Glutathione PeroxidaseFerroptosisLipoxygenaseReactive Oxygen Species (ROS)DNA/RNA SynthesisLOXCovalent inhibitorsGlutathione peroxidase 4Lipid peroxidationInhibitorinhibitorinhibit

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