2. PROTAC Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  3. Molecular Glues Glutathione Peroxidase Ferroptosis Reactive Oxygen Species (ROS)
  4. GPX4-IN-20

GPX4-IN-20 是一种 Arctigenin (HY-N0035) 衍生物，是 GPX4 的分子胶 (molecular glue) 降解剂，并通过增加脂质 ROS 水平和抑制 GSH 水平来诱导铁死亡 (ferroptosis)。GPX4-IN-20 以剂量依赖性方式降低 GPX4 的蛋白质表达和酶活性，而不影响其他与铁死亡相关的蛋白质。GPX4-IN-20 可诱导 GPX4 的泛素化依赖性蛋白酶体降解。GPX4-IN-20 还增加了 HCT-116 细胞中丙二醛 (MDA) 的水平。GPX4-IN-20 可用于结直肠癌的研究。

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GPX4-IN-20

GPX4-IN-20 Chemical Structure

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GPX4-IN-20 相关抗体

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GPX1 GPX4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GPX4-IN-20, a Arctigenin (HY-N0035) derived, is a GPX4& molecular gluedegrader. GPX4-IN-20 induces ferroptosis by increasing lipid ROS levels and suppressing GSH levels. GPX4-IN-20 reduces the protein expression and enzyme activity of GPX4 in a dose-dependent manner without affecting other ferroptosis-related proteins. GPX4-IN-20 induces ubiquitination-dependent proteasomal degradation of GPX4. GPX4-IN-20 also increases the level of malondialdehyde (MDA) in HCT-116 cells. GPX4-IN-20 can be used for the research of colorectal cancer[1].

体外研究
(In Vitro)

GPX4-IN-20 (2.5-10 μM；24-72 小时) (compound W25) 对 HCT-116 细胞具有细胞毒活性[1]。
GPX4-IN-20 (2.5-10 μM；24 小时；HCT-116 细胞) 抑制 GPX4 蛋白表达和活性，促进泛素化依赖的蛋白酶体降解。GPX4-IN-20 对铁死亡的其他关键调控因子，例如铁死亡抑制蛋白 1 (FSP1)、铁蛋白重链 1 (FTH1)、核受体共激活因子 4 (NCOA4) 和溶质载体家族 7 成员 11 (SLC7A11)，没有显著影响[1]。
GPX4-IN-20 (2.5-10 μM；24 小时；HCT-116 细胞) 不影响 GPX4 mRNA 水平[1]。
GPX4-IN-20 (0、2.5、5、10 μM；6 小时) 以剂量依赖的方式抑制 HCT-116 细胞的克隆形成[1]。
GPX4-IN-20 (24 h) 可抑制 HT-29 细胞的生长，IC50 值为 4.60 μM[1]。
GPX4-IN-20 (0, 2.5, 5, 10 μM；6, 12, 24 小时；HCT-116 细胞) 以剂量和时间依赖的方式显著增加 HCT-116 细胞中的脂质 ROS 水平。GPX4-IN-20 显著降低 GPX4 水平。GPX4-IN-20 处理后，细胞内 MDA 含量呈剂量依赖性增加[1]。 GPX4-IN-20 (10 μM；24 小时；HCT-116 细胞) 与 GPX4 结合并改变其热稳定性[1]。

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

GPX4-IN-20 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT-116 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: After HCT-116 cells were treated for 24, 48, and 72 h, the resulting IC50 values were 4.17 μM , 2.49 μM, and 2.24 μM, respectively.

Western Blot Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Inhibited the protein expression of GPX4 in a dose-dependent manner; suppressed the activity of GPX4; promoted the ubiquitination level of GPX4, inducing ubiquitination-dependent proteasomal degradation of GPX4.

Real Time qPCR[1]

Cell Line: HCT-116 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Did not significantly affect GPX4 mRNA levels in HCT-116 cells.
分子量

568.01

Formula

C30H30ClNO8
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-20 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

GPX4-IN-20Molecular GluesGlutathione PeroxidaseFerroptosisReactive Oxygen Species (ROS)Protein ubiquitinationGPX4molecular glueROSGSHMDAcolorectal cancerInhibitorinhibitorinhibit

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