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RSL3
CAS No. : 1219810-16-8
MCE 国际站:RSL3
产品活性:RSL3 ((1S,3R)-RSL3) 是一种谷胱甘肽过氧化物酶 4 (GPX4) 的抑制剂 (ferroptosis 激动剂),可降低 GPX4 的表达,诱导头颈部癌细胞的肥大性死亡。在 HN3 耐受细胞中,可增加 p62 和 Nrf2 的蛋白水平,使 Keap1 灭活。
研究领域:Autophagy | Apoptosis | Metabolic Enzyme/Protease | NF-κB | Immunology/Inflammation
作用靶点:p62 | Glutathione Peroxidase | Ferroptosis | Reactive Oxygen Species
In Vitro: RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC50s of 0.48 μM in HN3 and 5.8 μM in HN3-rslR cells, respectively.
RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
Ferroptosis-sensitive Cell Lines
Ferroptosis-sensitive Cells | Test Conditions |
MCF10A-RAS | 0-10 μM; 48 h |
MDA-MB-468 | 0.1-1 μM; 24 h |
PC-3 | 0.01-1 μM; 24 h |
Huh-7 | 0.01-1 μM; 24 h |
Raji | 0.01-1 μM; 24 h |
MEF | 0.1-100 nM; 24 h |
HT-22 neuron | 200 nM; 16 h |
NCI-H508 | 0.1-10 μM; 48 h |
LoVo | 0.1-10 μM; 48 h |
LS513 | 0.1-10 μM; 48 h |
SW480 | 0.1-10 μM; 48 h |
SW620 | 0.1-10 μM; 48 h |
SW1116 | 0.1-10 μM; 48 h |
DLD-1 | 0.1-10 μM; 48 h |
Caco-2 | 0.1-10 μM; 48 h |
HT-1080 | 0-10 μM; 48 h; IC50 1.55 μM |
MDA-MB-436 | 0.1-2 μM; 24 h |
HT-29 | 0.1-2 μM; 24 h |
U-373 | 0.1-2 μM; 24 h |
A549 | 1 nM-100 μM; 24 h; IC50 0.5 μM |
H1975 | 1 nM-100 μM; 24 h; IC50 150 nM |
MAD-MB-231 | 0-10 μM; 96 h; IC50 0.71 μM |
HCC1937 | 0-10 μM; 96 h; IC50 0.85 μM |
Ferroptosis-insensitive Cell Lines
Ferroptosis-insensitive Cells | Test Conditions |
HS578T | 0-2.5 μM; 24 h |
MCF10A | 0-2.5 μM; 24 h |
In Vivo: RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with Trigonelline (HY-N0414) in mice bearing HN3R cells.
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