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RSL3

Catalog No. T3646   CAS 1219810-16-8
Synonyms: RSL3 1S, 1S,3R-RSL3

RSL3 (RSL3 1S) 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).

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RSL3 Chemical Structure
RSL3, CAS 1219810-16-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 47.00
5 mg In stock $ 72.00
10 mg In stock $ 128.00
25 mg In stock $ 271.00
50 mg In stock $ 368.00
100 mg In stock $ 483.00
500 mg In stock $ 1,080.00
1 g In stock $ 1,430.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 99.96%
Purity: 99.64%
Purity: 99.39%
Purity: 98.06%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RSL3 (RSL3 1S) 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).
Targets&IC50 GSH:100 nM
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].
Cell Research 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)
Synonyms RSL3 1S, 1S,3R-RSL3
Molecular Weight 440.88
Formula C23H21ClN2O5
CAS No. 1219810-16-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 44.1 mg/mL (100 mM)

TargetMolReferences and Literature

1. Yang WS, et al. Chem Biol. 2008, 15(3):234-245. 2. Y Xie, et al. Cell Death and Differentiation. 2016, 23:369-379. 3. Li H, Shi W, Li X, et al. Ferroptosis is Accompanied by• OH Generation and Cytoplasmic Viscosity Increase Revealed via Dual-Functional Fluorescence Probe[J]. Journal of the American Chemical Society. 2019.

TargetMolCitations

1. Hu G, Cui Z, Chen X, et al.Suppressing Mesenchymal Stromal Cell Ferroptosis Via Targeting a Metabolism‐Epigenetics Axis Corrects their Poor Retention and Insufficient Healing Benefits in the Injured Liver Milieu.Advanced Science.2023: 2206439. 2. Feng Y, Luo X, Li Z, et al.A ferroptosis-targeting ceria anchored halloysite as orally drug delivery system for radiation colitis therapy.Nature Communications.2023, 14(1): 5083. 3. Bi G, Liang J, Shan G, et al.Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells.Cancer Research.2023: CAN-22-3977. 4. Li Y, Yang W, Zheng Y, et al.Targeting fatty acid synthase modulates sensitivity of hepatocellular carcinoma to sorafenib via ferroptosis.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 5. Wang X, Ji Y, Qi J, et al.Mitochondrial carrier 1 (MTCH1) governs ferroptosis by triggering the FoxO1-GPX4 axis-mediated retrograde signaling in cervical cancer cells.Cell Death & Disease.2023, 14(8): 1-13. 6. Tan Q, Zhang X, Li S, et al.DMT1 differentially regulates mitochondrial complex activities to reduce glutathione loss and mitigate ferroptosis.Free Radical Biology and Medicine.2023 7. Zhao G, Liang J, Shan G, et al.KLF11 regulates lung adenocarcinoma ferroptosis and chemosensitivity by suppressing GPX4.Communications Biology.2023, 6(1): 570. 8. Bow Y D, Ko C C, Chang W T, et al.A novel quinoline derivative, DFIQ, sensitizes NSCLC cells to ferroptosis by promoting oxidative stress accompanied by autophagic dysfunction and mitochondrial damage.Cancer Cell International.2023, 23(1): 1-11. 9. Gartzke L P, Hendriks K D W, Hoogstra-Berends F, et al.Inhibition of Ferroptosis Enables Safe Rewarming of HEK293 Cells following Cooling in University of Wisconsin Cold Storage Solution.International Journal of Molecular Sciences.2023, 24(13): 10939. 10. Jiang X, Teng X, Shi H, et al.Discovery and optimization of olanzapine derivatives as new ferroptosis inhibitors.Bioorganic Chemistry.2023: 106393.
11. Liu J, Meng F, Lv J, et al.Comprehensive Monitoring of Mitochondrial Viscosity Variation during Different Cell Death Processes by a NIR Mitochondria-targeting Fluorescence Probe.Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy.2023: 122602. 12. Li Y, Bao Y, Li Y, et al.RSL3 Inhibits Porcine Epidemic Diarrhea Virus Replication by Activating Ferroptosis.Viruses.2023, 15(10): 2080. 13. Shi H, Jiang X, Cao L, et al.Chemical constituents of Ajuga forrestii and their anti-ferroptosis activity.Fitoterapia.2023: 105461. 14. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 15. Peng, Xing, et al. Discovery of phloroglucinols from Hypericum japonicum as ferroptosis inhibitors. Fitoterapia. (2021): 104984. 16. Zhang H, Shan G, Jin X, et al. ARNTL2 is an indicator of poor prognosis, promotes epithelial-to-mesenchymal transition and inhibits ferroptosis in lung adenocarcinoma. Translational Oncology. 2022, 26: 101562. 17. Peng X, Tan Q, Wu L, et al. Ferroptosis Inhibitory Aromatic Abietane Diterpenoids from Ajuga decumbens and Structural Revision of Two 3, 4-Epoxy Group-Containing Abietanes. Journal of Natural Products. 2022 18. Wang F, Liu Y, Ni F, et al. BNC1 deficiency-triggered ferroptosis through the NF2-YAP pathway induces primary ovarian insufficiency. Nature Communications. 2022, 13(1): 1-17. 19. Li W, Luo L X, Zhou Q Q, et al. Phospholipid peroxidation inhibits autophagy via stimulating the delipidation of oxidized LC3-PE. Redox Biology. 2022: 102421. 20. Ning X, Qi H, Yuan Y, et al. Identification of a new small molecule that initiates ferroptosis in cancer cells by inhibiting the system Xc− to deplete GSH. European Journal of Pharmacology. 2022: 175304. 21. Fang Y, Tan Q, Zhou H, et al. Discovery and optimization of 2-(trifluoromethyl) benzimidazole derivatives as novel ferroptosis inducers in vitro and in vivo. European Journal of Medicinal Chemistry. 2022: 114905. 22. Li H, Shi W, Li X, et al. Ferroptosis is Accompanied by• OH Generation and Cytoplasmic Viscosity Increase Revealed via Dual-Functional Fluorescence Probe. Journal of the American Chemical Society. 2019 23. Shan G, Bi G, Zhao G, et al.Inhibition of PKA/CREB1 pathway confers sensitivity to ferroptosis in non-small cell lung cancer.Respiratory Research.2023, 24(1): 1-15. 24. Cao Z, Liu X, Zhang W, et al.Biomimetic Macrophage Membrane-Camouflaged Nanoparticles Induce Ferroptosis by Promoting Mitochondrial Damage in Glioblastoma.ACS nano.2023
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Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Ferroptosis Compound Library Anti-Aging Compound Library Glutamine Metabolism Compound Library Cysteine Covalent Library Inhibitor Library Bioactive Compound Library Anti-Cancer Active Compound Library Covalent Inhibitor Library Metabolism Compound Library

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Keywords

RSL3 1219810-16-8 Apoptosis Metabolism oxidation-reduction Ferroptosis GPX Glutathione Peroxidase inhibit RSL-3 (1S,3R)-RSL3 RSL3 1S 1S,3R-RSL3 Inhibitor RSL 3 inhibitor

 

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