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RSL3 Sale (Synonyms: (1S,3R)-RSL3)

Catalog No.GC12431 Copy One-Click Copy Product Info

RSL3, a GPX4 inhibitor, triggers lipid peroxidation and decreases GPX4 expression.

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RSL3 Chemical Structure

Cas No.: 1219810-16-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$88.00
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1mg
$35.00
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2mg
$60.00
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5mg
$93.00
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10mg
$147.00
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25mg
$239.00
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50mg
$351.00
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100mg
$502.00
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Sample solution is provided at 25 µL, 10mM.



Product has been cited by 18 publications

Description of RSL3

RSL3, a GPX4 inhibitor, triggers lipid peroxidation and decreases GPX4 expression[1]. RSL3 induces oxidative stress in glioma cells, upregulates glutathione S-transferase P1 (GSTP1), promotes S-glutathionylation of TGM2, and ultimately results in proteasomal degradation of TGM2, making glioma cells more sensitive to ionizing radiation[2]. RSL3 has been routinely used to elicit ferroptosis and induce apoptosis in various cancer cells[3].

In vitro, RSL3 treatment for 48 hours significantly inhibited the viability of 4T1 and MCF-7 cells, with IC50 values of 3.69μM and 13.57μM, respectively[4]. Treatment with 80nM RSL3 for 24 hours significantly induced cell death in MDA-MB-231 cells and decreased mitochondrial membrane potential[5]. Treatment with 5μM RSL3 for 12 hours promoted PARP1 cleavage and induced DNA damage in LoVo cells, while reducing cell proliferation[6].

In vivo, RSL3 treatment via daily intraperitoneal injection at a dose of 10mg/kg for 15 days significantly inhibited the growth of glioma cells in nude mice and induced glycolytic dysfunction[7]. Intratumoral injection of RSL3 at a dose of 100mg/kg every two weeks for 2 weeks significantly inhibited tumor growth in the U87 xenograft mouse model[8].

References:

[1] Yang W S, SriRamaratnam R, Welsch M E, et al. Regulation of ferroptotic cancer cell death by GPX4[J]. Cell, 2014, 156(1): 317-331.

[2] Wang X, Shi W, Li M, et al. RSL3 sensitizes glioma cells to ionizing radiation by suppressing TGM2-dependent DNA damage repair and epithelial-mesenchymal transition[J]. Redox Biology, 2024, 78: 103438.

[3] Liu L, Yang C, Zhu L, et al. RSL3 enhances ROS-mediated cell apoptosis of myelodysplastic syndrome cells through MYB/Bcl-2 signaling pathway[J]. Cell Death & Disease, 2024, 15(7): 465.

[4] Xu C, Xiao Z, Wang J, et al. Discovery of a potent glutathione peroxidase 4 inhibitor as a selective ferroptosis inducer[J]. Journal of Medicinal Chemistry, 2021, 64(18): 13312-13326.

[5] Feith M, Das Sajib S, Myrann A G, et al. Induction of Cell Death by Combined Treatment with Photosensitizer‐Chitosan Nanoparticles and the Ferroptosis Inducer RSL3 in Breast Cancer Cell Lines[J]. Advanced NanoBiomed Research, 2025, 5(5): 2400208.

[6] Chen D, Xie F, Mo Y, et al. RSL3 promotes PARP1 apoptotic functions by distinct mechanisms during ferroptosis[J]. Cellular & Molecular Biology Letters, 2025, 30(1): 109.

[7] Wang X, Lu S, He C, et al. RSL3 induced autophagic death in glioma cells via causing glycolysis dysfunction[J]. Biochemical and biophysical research communications, 2019, 518(3): 590-597.

[8] Li S, He Y, Chen K, et al. RSL3 drives ferroptosis through NF‐κB pathway activation and GPX4 depletion in glioblastoma[J]. Oxidative medicine and cellular longevity, 2021, 2021(1): 2915019.

Protocol of RSL3

Cell experiment [1]:

Cell lines

4T1 cells

Preparation Method

4T1 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS), and 1% penicillin-streptomycin at 37°C in 5% CO2/atmosphere. 4T1 cells were seeded onto 96-well microplates (5×103 cells/well) and cultured for 24h. Cells were treated with RSL3 at increasing concentrations (0, 0.01, 0.1, 1, 10, and 100μM) in the presence of 10% FBS for 48h, cell viability was assessed.

Reaction Conditions

0, 0.01, 0.1, 1, 10, and 100μM; 48h

Applications

RSL3 treatment reduced the cell viability of 4T1 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Athymic BALB/c nude mice

Preparation Method

Athymic BALB/c nude mice (4 weeks old; 20-22g) were housed under controlled temperature (21-23°C), humidity (30-35%) and light cycle (7:00 AM to 7:00 PM) and maintained on a standard rodent diet. A total of 1×106 logarithmically growing C6 cells in 100μl of PBS were subcutaneously injected into the right flank of each mouse. RSL3 treatment was started when the volume of tumors reached about 150mm3 after 7 days. The mice were allocated to receive intraperitoneal injections of vehicle (control group, n=10/group) and 10mg/kg RSL3 (n=10/group in each group) in the same volume 50μl once a day for 15 days. The tumor volume was calculated using the formula: 0.5×A×B2, in which A is the length of the tumor and B is the width.

Dosage form

10mg/kg/day; 15 days; i.p.

Applications

RSL3 treatment significantly inhibited tumor growth in mice with C6 xenografts.

References:

[1] Xu C, Xiao Z, Wang J, et al. Discovery of a potent glutathione peroxidase 4 inhibitor as a selective ferroptosis inducer[J]. Journal of Medicinal Chemistry, 2021, 64(18): 13312-13326.

[2] Wang X, Lu S, He C, et al. RSL3 induced autophagic death in glioma cells via causing glycolysis dysfunction[J]. Biochemical and biophysical research communications, 2019, 518(3): 590-597.

Chemical Properties of RSL3

Cas No. 1219810-16-8 SDF
Synonyms (1S,3R)-RSL3
Chemical Name (1S,3R)-methyl 2-(2-chloroacetyl)-1-(4-(methoxycarbonyl)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate
Canonical SMILES COC(C1=CC=C([C@@]2([H])C3=C(C4=CC=CC=C4N3)C[C@](N2C(CCl)=O)([H])C(OC)=O)C=C1)=O
Formula C23H21ClN2O5 M.Wt 440.88
Solubility ≥ 125.4 mg/mL in DMSO Storage Store at -20°C, sealed storage, away from moisture
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of RSL3

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2682 mL 11.341 mL 22.6819 mL
5 mM 453.6 μL 2.2682 mL 4.5364 mL
10 mM 226.8 μL 1.1341 mL 2.2682 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

Quality Control & SDS

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Quality Control

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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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