RSL3

Catalog No.S8155

RSL3 Chemical Structure

Molecular Weight(MW): 440.88

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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4 Customer Reviews

  • Fluvastatin treatment of HT-1080 cells decreases GPX4 protein levels in a time- and concentration-dependent manner and synergized with co-treatment with the direct GPX4 inhibitor RSL3.

    Nature, 2017, 547(7664):453-457. RSL3 purchased from Selleck.

    HK2 cells with elevated PEBP1 are more sensitive to ferroptosis. Inset: ferrostatin-1-inhibitable cell death (means ± SD, *p < 0.05 versus pCMV6, **p < 0.05 versus pCMV6/RSL3, ***p < 0.05 versus pCMV6-PEBP1/RSL3, #p < 0.05 versus pCMV6/RSL3, n = 3/group). Inset: quantitation of ferroptosis as differences in LDH in ± FER-treated cells.

    Cell, 2017, 171(3):628-641. RSL3 purchased from Selleck.

  • ATG3 is required for ferroptosis. ATG3KO MEFs, or ATG3KO cells reconstituted with ectopic ATG3 expression, were treated as indicated for 12 h. Cell death was determined by PI staining coupled with flow cytometry. ATG3 expression was confirmed by immunoblotting. erastin: 1 μM; RSL3: 1 μM.

    Cell Res, 2016, 26(9):1021-32. RSL3 purchased from Selleck.

    (D) Representative western blot and (E) densitometry showing protein levels of HO-1 in HO-1+/+ PTCs treated with RSL3 over time. Data shown represent the Mean ± SEM of three independent experiments performed each time in triplicate; * = p<0.05, ** = p<0.01 compared to lower concentration at each time point.

    Am J Physiol Renal Physiol, 2017, doi: 10.1152/ajprenal.00044.2017. RSL3 purchased from Selleck.

Purity & Quality Control

Choose Selective Ferroptosis Inhibitors

Biological Activity

Description 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.
Targets
Gpx4 [1]
(In Calu-1 cells)
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].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: TERT/LT/ST/RASV12 cells 
  • Concentrations: 1 µg/ml
  • Incubation Time: 16hrs
  • Method:

    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)
Animal Research:

[1]

+ Expand
  • Animal Models: athymic nude mice(8 weeks)implanted with subcutaneous xenograft tumors derived from BJeLR cells
  • Formulation: --
  • Dosages: 100 mg/kg
  • Administration: s.c. injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.6 mM)
Ethanol 22 mg/mL (49.9 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
2mg/mL

* 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.

Chemical Information

Molecular Weight 440.88
Formula

C23H21ClN2O5

CAS No. 1219810-16-8
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID