RSL3
| Code | Size | Price |
|---|
| TAR-T3646-1mg | 1mg | £98.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| TAR-T3646-2mg | 2mg | £109.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| TAR-T3646-5mg | 5mg | £130.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| TAR-T3646-10mg | 10mg | £178.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T3646-25mg | 25mg | £288.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T3646-50mg | 50mg | £438.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T3646-100mg | 100mg | £459.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
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).
Biological Applications:
RSL3 and Erastin, as activators of ferroptosis, can induce cellular ferroptosis. Ferroptosis can be employed to eliminate problematic cell types, such as cancer cells, inflammatory cells, or activated fibroblasts. Abundant research indicates that ferroptosis plays a crucial role in various conditions such as tumor suppression, immunity, neurodegenerative diseases, tissue and organ damage, inflammatory and infectious diseases. Scientists widely believe that targeting ferroptosis holds the potential to advance the development and clinical translation of therapies based on ferroptosis.
CAS:
1219810-16-8
Description:
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).
Formula:
C23H21ClN2O5
Mechanism of Action:
Ferroptosis is a type of programmed cell death different from apoptosis and necrotic cell death. Actually, ferroptosis is characterized by the depletion of glutathione (GSH), a reduction in the activity of glutathione peroxidase 4 (GPX4), and the iron-dependent accumulation of reactive oxygen species (ROS) and lipid ROS.
Ferroptosis can be triggered by various small molecules, including RSL3 and Erastin, which directly inhibit the cystine/glutamate reverse transporter protein (System Xc-) on the cell surface and GPX4. The cystine/glutamate reverse transporter protein is a heterodimer on the cell membrane responsible for the intracellular and extracellular transport of cystine and glutamate. It facilitates a 1:1 exchange of cystine and glutamate in and out of the cell. Absorbed cystine is reduced to cysteine within the cell, and cysteine, along with glutamate, is utilized in the biosynthesis of reduced glutathione (GSH). GSH, under the action of GPX4, reduces lipid hydroperoxides to lipid alcohols, thereby reducing ROS. Inhibiting the activity of System Xc- can affect GSH synthesis, leading to reduced GPX4 activity, diminished cellular antioxidant capacity, accumulation of lipid ROS, and ultimately resulting in oxidative damage and ferroptosis.
Molecular Weight:
440.88
Pathway:
Cell Cycle/Checkpoint; oxidation-reduction; Apoptosis; Metabolism
Purity:
0.9964
Research Area:
Tumour suppression and immunity; Neurodegenerative diseases; Tissue and organ damage; Inflammatory and infectious diseases
SMILES:
COC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H](N1C(=O)CCl)c1ccc(cc1)C(=O)OC
Target:
Ferroptosis; GPX; Glutathione Peroxidase
References
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.
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.
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
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.
Y Xie, et al. Cell Death and Differentiation. 2016, 23:369-379.
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.
Yang WS, et al. Chem Biol. 2008, 15(3):234-245.
Zhao G, Liang J, Shan G, et al.KLF11 regulates lung adenocarcinoma ferroptosis and chemosensitivity by suppressing GPX4.Communications Biology.2023, 6(1): 570.
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.
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.
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.
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.
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.
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
Li Y, Bao Y, Li Y, et al.RSL3 Inhibits Porcine Epidemic Diarrhea Virus Replication by Activating Ferroptosis.Viruses.2023, 15(10): 2080.
Shi H, Jiang X, Cao L, et al.Chemical constituents of Ajuga forrestii and their anti-ferroptosis activity.Fitoterapia.2023: 105461.
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.
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.
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.
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.
Jiang X, Teng X, Shi H, et al.Discovery and optimization of olanzapine derivatives as new ferroptosis inhibitors.Bioorganic Chemistry.2023: 106393.
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
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.
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.
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.
Peng, Xing, et al. Discovery of phloroglucinols from Hypericum japonicum as ferroptosis inhibitors. Fitoterapia. (2021): 104984.