RSL3 ((1S,3R)-RSL3) 是一种谷胱甘肽过氧化物酶 4 (GPX4) 的抑制剂,可降低 GPX4 的表达,诱导头颈部癌细胞的铁死亡 (ferroptosis 激动剂)。在 HN3 耐受细胞中,可增加 p62 和 Nrf2 的蛋白水平,使 Keap1 失活。
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产品名称 | Ferroptosis ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ferrostatin-1 |
++
Ferroptosis, EC50: 60 nM |
98% | |||||||||||||||||
Liproxstatin-1 |
+++
ferroptosis, IC50: 22 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | RSL3, also known as (1S,3R)-RSL3, acts as an inhibitor of glutathione peroxidase 4 (GPX4), which is a ferroptosis activator. It diminishes the GPX4 protein levels and prompts ferroptotic cell death in head and neck cancer cells. Additionally, RSL3 elevates the levels of p62 and Nrf2 and deactivates Keap1 in HN3-rslR cells[1]. RSL3, within concentration of 8 μM over 72 hours, significantly decreases the viability of HN3 cells. The IC50 values are 0.48 μM for HN3 cells and 5.8 μM for HN3-rslR cells, respectively. RSL3, in concentrations ranging from 0 to 8 μM over a period of 24 hours, diminishes GPX4 protein levels, augments the expression of p62 and Nrf2, and deactivates Keap1 in HN3-rslR cells[1]. |
Animal study | Administering RSL3 at a dosage of 100 mg/kg, intratumorally twice per week for a duration of 20 days, notably hampers tumor growth when used alongside Trigonelline in mice implanted with HN3R cells[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.27mL 0.45mL 0.23mL |
11.34mL 2.27mL 1.13mL |
22.68mL 4.54mL 2.27mL |
CAS号 | 1219810-16-8 |
分子式 | C23H21ClN2O5 |
分子量 | 440.88 |
SMILES Code | O=C([C@H]1CC2=C([C@H](C3=CC=C(C(OC)=O)C=C3)N1C(CCl)=O)NC4=C2C=CC=C4)OC |
MDL No. | MFCD30187526 |
别名 | (1S,3R)-RSL3 |
运输 | 蓝冰 |
InChI Key | TXJZRSRTYPUYRW-NQIIRXRSSA-N |
Pubchem ID | 1750826 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
溶解方案 |
DMSO: 105 mg/mL(238.16 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 2.4 mg/mL clear PO 0.5% CMC-Na 28 mg/mL suspension |