RSL3
作者：齊岳
發(fā)布時(shí)間：2023-09-07
09:28:10
點(diǎn)擊數(shù)：
產(chǎn)品名稱：RSL3
產(chǎn)品描述：
| 產(chǎn)品描述 | RSL3 is a VDAC-independent ferroptosis activator with selectivity for tumor cells bearing oncogenic RAS. RSL3 is the inhibitor of the glutathione peroxidase 4, which can inhibit the cysteine/glutamate amino acid transporter system xc- that blocks GSH synthesis (IC50: 100 nM). | ||||||||||||||||
| 靶點(diǎn)活性 | GSH:100 nM | ||||||||||||||||
| 體外活性 | 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[1][2].
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| 體內(nèi)活性 | 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[1].
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| 細(xì)胞實(shí)驗(yàn) | TERT/LT/ST/RASV12 cells are seeded in 10 cm dishes and treated with 1 µM staurosporine, 10 µg/ml erastin, 20 µg/ml RSL5, and 1 µg/ml RSL3 for 16 hr. Both dying cells and live cells in each 10 cm dish are harvested and collected in the same 15 ml tubes by centrifuging cell suspension at 1000 rpm for 5 min. (Only for Reference) |
| 別名 | RSL3 1S, 1S,3R-RSL3 |
| 化合物與蛋白結(jié)合的復(fù)合物 |
Crystal structure of human GPX4-U46C in complex with RSL3 |
| 分子量 | 440.88 |
| 分子式 | C23H21ClN2O5 |
| CAS No. | 1219810-16-8 |
存儲(chǔ)
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 44.1 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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