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Cat. No. | Product Name | Target | Signaling Pathways |
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T77755 |
GPX4-IN-5
|
GPX | oxidation-reduction |
GPX4-IN-5 是一种小分子共价 GPX4 抑制剂(IC50: 0.12 μM),具有抗肿瘤活性。GPX4-IN-5 可促使铁死亡,可用于预防和治疗三阴性乳腺癌 (TNBC)。 | |||
T77759 |
GPX4-IN-6
|
GPX | oxidation-reduction |
GPX4-IN-6 是一种小分子共价 GPX4 抑制剂(IC50: 0.12 μM),具有抗肿瘤活性。GPX4-IN-6 可促使铁死亡,用于治疗=和预防三阴性乳腺癌 (TNBC)。 | |||
T36935 |
PKUMDL-LC-101-D04
GPX4-Activator-1d4,PKUMDL-LC-101-D04 |
GPX | oxidation-reduction |
PKUMDL-LC-101-D04是一种高效的谷胱甘肽过氧化物酶4(GPX4)的异位激活剂,是一种铁死亡的调节剂。 当在无细胞试验中使用浓度为20 μM 时,GPX4活性增加到对照水平的150%;在野生型而非Gpx4-/-小鼠胚胎成纤维细胞(MEF)提取物中使用浓度为61 μM 时,GPX4活性增加到对照水平的150%。PKUMDL-LC-101-D04(200 μM)能减少胆固醇过氧化氢诱导的MEF 死亡。 | |||
T83780 |
GPX4 24
Phospholipid Hydroperoxide Glutathione Peroxidase 24,PHGPx 24,Glutathione Peroxidase 4 24 |
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GPX4 24是(1S,3R)-RSL3的衍生物,具有抑制谷胱甘肽过氧化物酶4(GPX4)的作用。它能够在浓度依赖的方式中与4T1小鼠乳腺癌细胞中的GPX4形成共价结合。在GPX4依赖的HT-1080成纤维细胞中,GPX4 24诱导铁死亡(EC50 = 0.16 µM)。当以200 mg/kg剂量给予小鼠时,它能够增加小鼠肾脏和血浆中丙二醛(MDA)的水平。 | |||
T74846 | GPX4-IN-4 | Glutathione Peroxidase | Metabolism |
GPX4-IN-4(Compound 24)作为一种GPX4抑制剂,具有显著效能,主要应用于癌症领域的科学研究。 | |||
T74796 | PROTAC GPX4 degrader-1 | ||
PROTACGPX4 degrader-1 (DC-2) 是GPX4的PROTAC 降解剂,其在HT1080 细胞中的DC50值为 0.03 μM。 | |||
T63729 |
GPX4-IN-3
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GPX4-IN-3 (26a) 作为一种有效的谷胱甘肽过氧化物酶4 (GPX4) 抑制剂,其能选择性诱导铁死亡(ferroptosis)。在1 μM浓度下,该化合物能抑制GPX4活性达71.7%。 | |||
T79777 |
GPX4-IN-7
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Ferroptosis | Apoptosis |
GPX4-IN-7 (Compound 31),一种靛玉红衍生物,作为结肠癌铁死亡的诱导剂,对HCT-116细胞显示出卓越的抗肿瘤效果,IC50为0.49 μM。该化合物通过促进GPX4降解和脂质ROS积累,有效触发铁死亡。 | |||
T73235 | GPX4-IN-2 | ||
GPX4-IN-2 是一种有效的 GPX4抑制剂。GPX4 显示出抗增殖活性。GPX4-IN-2具有癌症研究的潜力。 | |||
T4066 |
FIN56
|
Ferroptosis | Apoptosis |
FIN56 是一种铁死亡特异性诱导剂,能结合并激活角鲨烯合酶,可通过诱导 GPX4 降解来诱导铁死亡。 | |||
T8970 |
ML162
|
Ferroptosis; GPX; Glutathione Peroxidase | Apoptosis; Metabolism; oxidation-reduction |
ML162 是一种共价谷胱甘肽过氧化物酶 4 抑制剂。它选择性抑制表达突变 RAS 癌基因的细胞系。 | |||
T11631 |
iFSP1
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Ferroptosis | Apoptosis |
iFSP1 是一种强效、选择性和谷胱甘肽独立的铁死亡抑制蛋白 1 (FSP1) (AIFM2) 抑制剂,具有EC50 为 103 nM。它能够使多种人类癌细胞系对铁死亡诱导剂敏感,例如 (1S,3R)-RSL3。它在过表达 FSP1 的 GPX4 敲除细胞中选择性地诱导铁死亡。 | |||
T8375 |
ML-210
CID 49766530 |
Ferroptosis; GPX; Glutathione Peroxidase; Ras | Apoptosis; GPCR/G Protein; MAPK; Metabolism; oxidation-reduction |
ML-210 (CID 49766530) 是一种共价的选择性谷胱甘肽过氧化物酶 4 (GPX4) 抑制剂,EC50为 30 nM。它与 GPX4 硒代半胱氨酸残基结合,具有抗癌活性。 | |||
T37314 |
JKE-1674
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GPX | oxidation-reduction |
JKE-1674 是口服有效的谷胱甘肽过氧化物酶 4 (GPX4)抑制剂,是ML-210的活性代谢物,ML-210也是GPX4抑制剂。它可转换成丁腈氧化物 JKE-1777。它用与 ML-210 相同的方式杀死 LOX-IMVI 细胞,并被ferroptosis 抑制剂完全挽救。 | |||
T3646 |
RSL3
RSL3 1S,1S,3R-RSL3 |
Ferroptosis; GPX; Glutathione Peroxidase | Apoptosis; Metabolism; oxidation-reduction |
RSL3 (RSL3 1S) 是一种 GPX4 的抑制剂,抑制阻断 GSH 合成的 system xc- (IC50=100 nM)。RSL3 是一种不依赖 VDAC 的铁死亡激活剂,对携带致癌 RAS 的肿瘤细胞具有选择性。 | |||
T77745 |
N6F11
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GPX | oxidation-reduction |
N6F11是一种新型且具有选择性和有效性的铁死亡诱导剂,具有抗癌抗肿瘤活性,通过与癌细胞中的TRIM25结合从而促进GPX4降解。N6F11 可用于研究胰腺癌。 | |||
T60084 |
FINO2
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Ferroptosis | Apoptosis |
FINO2作为一种强效的铁死亡诱导化合物,能够抑制GPX4活性。该化合物作为稳定的氧化剂,有效氧化亚铁并在不同pH水平下表现出稳定性。此外,FINO2诱导广泛的脂质过氧化。 | |||
T79294 |
NC-R17
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Glutathione Peroxidase | Metabolism |
NC-R17是一种衍生自RSL3的非共价GPX4降解剂,涉及铁死亡(Ferroptosis)过程。该化合物展现出抗肿瘤活性,用于非共价GPX4 PROTAC的设计。 | |||
T37805 |
JKE-1716
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JKE-1716 is an inhibitor of glutathione peroxidase 4 (GPX4) and a derivative of the GPX4 inhibitor ML-210 .1JKE-1716 reduces viability of LOX-IMVI cancer cells in a concentration-dependent manner and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1 . 1.Eaton, J.K., Furst, L., Ruberto, R.A., et al.Selective covalent targeting of GPX4 using masked nitrile-oxide electrophilesNat. Chem. Biol.16(5)497-506(2020) | |||
T62827 |
BCP-T.A
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BCP-T.A 是一种杂环亲电子试剂,能够结合 GPX4,进而有效诱导铁死亡 (ferroptosis)。 | |||
T79639 | Lepadin H | Ferroptosis | Apoptosis |
Lepadin H 是一种具有显著细胞毒性的海洋生物碱,能够诱导铁死亡。它通过增加 p53 表达、提升 ROS 生成和脂质过氧化来展开作用,同时抑制 SLC7A11 和 GPX4,上调 ACSL4。Lepadin H 主要通过 p53-SLC7A11-GPX4 路径实现其诱导铁死亡的功能。 | |||
T79638 | Lepadin E | Glutathione Peroxidase | Metabolism |
Lepadin E 是一种铁死亡(ferroptosis)诱导剂,它通过激活 p53-SLC7A11-GPX4 途径显著诱发细胞毒性。该化合物增强 p53 的表达,减少 SLC7A11 及 GPX4 的水平,进而导致活性氧 (ROS) 和脂质过氧化物的增加,并通过上调 ACSL4 来促进细胞死亡。Lepadin E 还具有显著的抗肿瘤效果。 | |||
T68239 |
NPD4928
|
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NPD4928 enhanced the sensitivity of various cancer cells to GPX4 inhibitors, suggesting that the combination might have therapeutic potential via the induction of ferroptosis. | |||
T79388 |
Anticancer agent 154
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Reactive Oxygen Species | Immunology/Inflammation; Metabolism; NF-κB |
Anticanceragent 154 (Compound 8h) 增加活性氧水平、导致线粒体损伤,并诱导细胞凋亡和 DNA 损伤。此外,该化合物通过降低 GSH 和 GPX4 水平,增加脂质过氧化,进而诱导铁死亡。Anticanceragent 154 对多种癌细胞株(HT29、H1975、A549 及 MCF-7)显示抑制作用,IC50 值在 1.0-1.9 μM 范围。 | |||
T36516 |
RC574
RC574 |
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RC574 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It inhibits glutamate-induced cell death in HT22 cells (IC50= 276.2 nM) and mouse primary cortical neurons when used at a concentration of 3 μM. RC574 (3 μM) increases glutathione peroxidase 1 (GPX1) levels and GPX activity, as well as inhibits glutamate-induced mitochondrial superoxide anion production, in HT22 cells. It completely inhibits ferroptosis induced by the GPX4 inhibitor ... | |||
T83886 |
icFSP1 TFA
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icFSP1是一种抑制剂,针对的是铁死亡抑制蛋白1(FSP1)。在2.5 µM的浓度下使用时,能够引发FSP1在细胞中的凝聚和相分离,但在无细胞测试中并不抑制FSP1的酶活性(IC50 = > 30 µM)。icFSP1以浓度依赖的方式诱导HT-1080纤维肉瘤细胞的铁死亡。在体内,icFSP1(50 mg/kg)通过使用人类过表达FSP1,Gpx4-/-Fsp1-/-的B16/F10细胞,在B16/F10鼠黑色素瘤模型中减少肿瘤体积和重量。 | |||
T37487 |
1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE
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1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE is a phospholipid that contains stearic acid at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3. | |||
T36515 | RC363 | ||
RC363 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It reduces 2,2-diphenyl-1-picrylhydrazyl radicals by approximately 40% in a cell-free assay when used at a concentration of 25 μM. RC363 prevents glutamate-induced toxicity in HT22 cultured hippocampal cells (IC50= 234.5 nM) but does not reduce oxidant levels in these cells. It increases the levels of glutathione peroxidase 1 (GPX1) and the activity of GPX in glutamate-challenged HT2... | |||
T36514 |
QD-394
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QD-394 is an inducer of reactive oxygen species (ROS) production.1It induces lipid peroxidation, increases in intracellular accumulation of reactive oxygen species (ROS), and decreases in the reduced glutathione (GSH) to oxidized GSH (GSSG) ratio in MIA PaCa-2 pancreatic cancer cells when used at concentrations ranging from 0.5 to 10 μM. QD-394 is cytotoxic to MIA PaCa-2, PANC-1, and BxPC-3 cancer cells (IC50s = 0.64, 0.34, and 0.9 μM, respectively). QD-394 acts synergistically with napabucasin ... |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN5770 |
Gingerenone A
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Nrf2 | Immunology/Inflammation |
Gingerenone A 是一种有效的 Nrf2-Gpx4 激活剂,是从生姜里面分离出来的小分子化合物,具有抗癌活性,可延长癌细胞的细胞周期,可抑制右旋糖酐硫酸钠 (DSS) 诱导的结肠炎小鼠继发性肝损伤 (SLI) 中的铁死亡。 |