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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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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。
用途
1S,3R-RSL 3已用于:
研究其作为谷胱甘肽过氧化物酶4(GPX4)抑制剂,对脑室下区多形性胶质母细胞瘤(GBM)细胞死亡的影响
研究其作为GPX4抑制剂和铁死亡诱导剂对小鼠心肌细胞死亡和心功能衰竭的影响
在细胞活力检测中作为HT-1080细胞铁死亡诱导剂
Information
RSL3 RSL3 ((1S,3R)-RSL3) is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS. RSL3 binds, inactivates GPX4 and thus mediates GPX4-regulated ferroptosis.
In vitro
Ferroptosis-inducing compounds inactivate GPX4 by direct binding or by depleting glutathione.After binding to GPX4, RSL3 inactivates GPX4 to induce ROS production from lipid peroxidation. RSL3\'s ability to induce synthetic lethality with oncogenic RAS is rapid and quite potent. This compound inhibits the growth of BJ-TERT/LT/ST/RASV12 and DRD cells as low as 10 ng/mland started to kill sensitive cells as early as 8 hr after treatment.
In vivo
Prostaglandin-endoperoxide synthase (PTGS) is the key enzyme in prostaglandin biosynthesis. There are two isozymes of PTGS: a constitutive PTGS1 and an inducible PTGS2. PTGS2 encoding cyclooxygenase-2 (COX-2) is significantly upregulated after treatment with RSL3 and erastin in mice.
Cell Data
cell lines:MOLT-4 cell lines and Reh (pre-B cells)
Concentrations:1 µg/ml
Incubation Time:16hrs
Powder Purity:≥99%