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Synonyms | (1S,3R)-RSL3 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H21ClN2O5 |
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分子量 | 440.88 | CAS No. | 1219810-16-8 | |
Solubility (25°C)* | 体外 | DMSO | 88 mg/mL (199.6 mM) | |
Ethanol | 6 mg/mL (13.6 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 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. |
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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[1][2]. |
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[1]. |
細胞アッセイ | 細胞株 | TERT/LT/ST/RASV12 cells |
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濃度 | 1 µg/ml | |
反応時間 | 16hrs | |
実験の流れ | 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. |
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動物実験 | 動物モデル | athymic nude mice(8 weeks)implanted with subcutaneous xenograft tumors derived from BJeLR cells |
投薬量 | 100 mg/kg | |
投与方法 | s.c. injection |
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, , Am J Physiol Renal Physiol, 2017, doi: 10.1152/ajprenal.00044.2017
Data from [Data independently produced by , , Nature, 2017, 547(7664):453-457]
Data from [Data independently produced by , , Cell, 2017, 171(3):628-641]
7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] | PubMed: 38297130 |
Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429] | PubMed: 38365899 |
Targeting of vulnerabilities of drug-tolerant persisters identified through functional genetics delays tumor relapse [ Cell Rep Med, 2024, 5(3):101471] | PubMed: 38508142 |
Dibutyl phthalate exposure induced mitochondria-dependent ferroptosis by enhancing VDAC2 in zebrafish ZF4 cells [ Environ Pollut, 2024, 348:123846] | PubMed: 38548160 |
Novel SK channel positive modulators prevent ferroptosis and excitotoxicity in neuronal cells [ Biomed Pharmacother, 2024, 171:116163] | PubMed: 38242037 |
PKCiota Inhibits the Ferroptosis of Esophageal Cancer Cells via Suppressing USP14-Mediated Autophagic Degradation of GPX4 [ Antioxidants (Basel), 2024, 13(1)114] | PubMed: 38247539 |
POU6F1 promotes ferroptosis by increasing lncRNA-CASC2 transcription to regulate SOCS2/SLC7A11 signaling in gastric cancer [ Cell Biol Toxicol, 2024, 40(1):3] | PubMed: 38267746 |
Astragaloside IV ameliorates cisplatin-induced liver injury by modulating ferroptosis-dependent pathways [ J Ethnopharmacol, 2024, 328:118080] | PubMed: 38521426 |
Oncolytic Newcastle disease virus induced degradation of YAP through E3 ubiquitin ligase PRKN to exacerbate ferroptosis in tumor cells [ J Virol, 2024, 98(3):e0189723] | PubMed: 38411946 |
Inhibition of ferroptosis by POLE2 in gastric cancer cells involves the activation of NRF2/GPX4 pathway [ J Cell Mol Med, 2024, 28(1):e17983] | PubMed: 38070189 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。