PROTAC GPX4 degrader-1

• 常用名: PROTAC GPX4 degrader-1
• 英文名: PROTAC GPX4 degrader-1
• CAS号: 2916433-81-1
• 分子量: 993.50
• 密度: N/A
• 沸点: N/A
• 分子式: C₅₀H₅₇ClN₁₀O₁₀
• 熔点: N/A
• 闪点: N/A

PROTAC GPX4 degrader-1用途

PROTAC GPX4降解器-1(DC-2)是一种基于PROTAC的GPX4去除器,在HT1080细胞中的DC50为0.03μM[1]。

PROTAC GPX4 degrader-1名称

• 英文名: PROTAC GPX4 degrader-1

PROTAC GPX4 degrader-1生物活性

• 描述: PROTAC GPX4降解器-1(DC-2)是一种基于PROTAC的GPX4去除器,在HT1080细胞中的DC50为0.03μM[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞凋亡 >> Ferroptosis
  信号通路 >> 蛋白裂解靶向嵌合体 >> PROTAC
• 体外研究: 已发现PROTAC GPX4降解剂-1(DC-2)可诱导GPX4的降解和随后的脱铁[1]。西方印迹分析[1]。细胞系：HT1080细胞。浓度：0.003-1μM。孵育时间：24小时。结果：GPX4蛋白水平呈剂量依赖性降解。
• 参考文献:

  [1]. Han Wang, et al. Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells. Eur J Med Chem. 2023 Jun 5;254:115343.

PROTAC GPX4 degrader-1物理化学性质

• 分子式: C₅₀H₅₇ClN₁₀O₁₀
• 分子量: 993.50
• InChIKey: HMSNFNLFZRKDIO-UHFFFAOYSA-N
• SMILES: Cc1onc(C(=O)N2CCN(C(c3ccc(Cl)cc3)c3ccc(OCC(=O)N4CCC(CN5CCN(CCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)cc3)CC2)c1[N+](=O)[O-]

PROTAC GPX4 degrader-1靶点实验

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实验名称：Induction of ferroptosis in human HT-1080 cells assessed as increase in ROS accumulat... 来源：ChEMBL 靶标：HT-1080 External Id：CHEMBL5327092

实验名称：PROTAC activity at CRBN/GPX4 in human HT-1080 cells assessed as induction of GPX4 deg... 来源：ChEMBL 靶标：Phospholipid hydroperoxide glutathione peroxidase GPX4 External Id：CHEMBL5327090

实验名称：Induction of ferroptosis in human HT-1080 cells assessed as cell death at 0.3 uM prei... 来源：ChEMBL 靶标：HT-1080 External Id：CHEMBL5327091

实验名称：PROTAC activity at CRBN/GPX4 in human HT-1080 cells assessed as induction of GPX4 deg... 来源：ChEMBL 靶标：Phospholipid hydroperoxide glutathione peroxidase GPX4 External Id：CHEMBL5327088

实验名称：PROTAC activity at CRBN/GPX4 in human HT-1080 cells assessed as induction of GPX4 deg... 来源：ChEMBL 靶标：Phospholipid hydroperoxide glutathione peroxidase GPX4 External Id：CHEMBL5327089

实验名称：Toxicity in Balb/c nude mouse xenografted with human HT-1080 cells assessed as body w... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5327086

实验名称：Potency index, ratio of test compound IC50 to ML210 IC50 for cytotoxicity against HEK... 来源：ChEMBL 靶标：HEK-293T External Id：CHEMBL5327084

实验名称：In vivo PROTAC activity at CRBN/GPX4 in human HT-1080 cells xenografted in Balb/c nud... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL5327085

实验名称：Antiproliferative activity against human HT-1080 cells assessed as reduction in cell ... 来源：ChEMBL 靶标：HT-1080 External Id：CHEMBL5327080

实验名称：PROTAC activity at CRBN/GPX4 in human HT-1080 cells assessed as induction of GPX4 deg... 来源：ChEMBL 靶标：Phospholipid hydroperoxide glutathione peroxidase GPX4 External Id：CHEMBL5327078

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