2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Glutathione Peroxidase Ferroptosis Reactive Oxygen Species (ROS)
  4. GPX4 degrader-1

GPX4 degrader-1 (Compound RS-1) 是一种基于疏水标签 (HyT) 技术的 GPX4 降解剂 (HT1080 细胞中 DC50：8.9 nM)。GPX4 degrader-1 可诱导 GPX4 降解，诱导铁死亡 (Ferroptosis)，并提升脂质 ROS 水平。GPX4 degrader-1 在小鼠乳腺癌模型中展现出强效抗肿瘤活性。

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GPX4 degrader-1

GPX4 degrader-1 Chemical Structure

CAS No. : 3057531-85-5

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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 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model[1].

IC50 & Target[1]

GPX4

8.9 nM (DC50)

体外研究
(In Vitro)

GPX4 degrader-1 (0.3-300 nM; 2-48 h) 可在 HT1080 纤维肉瘤细胞中诱导呈剂量和时间依赖性的蛋白酶体介导的 GPX4 降解，其 DC50 为 8.9 nM[1]。
GPX4 degrader-1 (48 h) 可在 HT1080、A549 和 4T1 癌细胞中诱导铁死亡介导的抗增殖活性，其 IC50 值分别为 130 nM、6.4 μM 和 700 nM[1]。
GPX4 degrader-1 (对于 MDA，0.5-2.0 μM ; 24-48 h) 可升高 HT1080 纤维肉瘤细胞中的脂质 ROS 和 MDA[1]。

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

GPX4 degrader-1 相关抗体:
体内研究
(In Vivo)

GPX4 degrader-1 (16-66 μmol/kg；腹腔注射；每日一次；10 天) 在 4T1 小鼠乳腺癌模型中实现了强效的、剂量依赖性的肿瘤生长抑制[1]。

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

Animal Model: BALB/c (female, 6 to 8 weeks old)[1]
Dosage: 16 μmol/kg; 33 μmol/kg; 66 μmol/kg
Administration: i.p.; daily; 10 days
Result: Induced dose-dependent tumor growth inhibition: 29.3% TGI at 16 μmol/kg, 54.6% TGI at 33 μmol/kg, and 80.5% TGI at 66 μmol/kg.
Demonstrated statistically significant superior antitumor activity compared to RSL3 at 66 μmol/kg (P < 0.01).
Reduced tumor weight in a dose-dependent manner.
Caused no significant changes in mouse body weight during the treatment period.
分子量

634.16

Formula

C38H36ClN3O4
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 degrader-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

GPX4 degrader-13057531-85-5Glutathione PeroxidaseFerroptosisReactive Oxygen Species (ROS)HT1080 fibrosarcoma cellsubiquitin-proteasome systemferroptosisGPX4reactive oxygen speciesmalondialdehydeA549 cancer cells4T1 cancer cellslipid peroxidationmurine mammary carcinoma modelInhibitorinhibitorinhibit

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