1. Metabolic Enzyme/Protease
    Apoptosis
  2. Glutathione Peroxidase
    Ferroptosis
  3. RSL3

RSL3 (Synonyms: (1S,3R)-RSL3)

Cat. No.: HY-100218A Purity: 99.95%
Handling Instructions

RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.

For research use only. We do not sell to patients.

RSL3 Chemical Structure

RSL3 Chemical Structure

CAS No. : 1219810-16-8

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Customer Review

Based on 17 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RSL3 purchased from MCE. Usage Cited in: Brain Res Bull. 2020 Jul 14;S0361-9230(20)30558-X.

    Gpx4 and 4-HNE expression assessment by Western blotting after RSL3 treatment. Western blot analysis reveal that compared with the Mel group, the RSL3 group has significantly decreased and increased Gpx4 and 4-HNE expression, respectively.

    RSL3 purchased from MCE. Usage Cited in: Brain Res Bull. 2020 Jul 14;S0361-9230(20)30558-X.

    Representative images and NeuN + cell quantification in the hippocampus via immunohistochemistry after RSL3 treatment. Compared with the Mel group, the RSL3 group has a significantly decreased NueN + cell number.
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    Description

    RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells[1].

    IC50 & Target

    Glutathione peroxidase 4[1]

    In Vitro

    RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC50s of 0.48 µM in HN3 and 5.8 µM in HN3-rslR cells, respectively[1].
    RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells[1].

    Cell Viability Assay[1]

    Cell Line: HN3 cells, HN3-rslR cells
    Concentration: 0-8 μM
    Incubation Time: 72 hours
    Result: Showed IC50s of 0.48 µM in HN3 and 5.8 µM in HN3-rslR cells, respectively[1].

    Western Blot Analysis[1]

    Cell Line: HN3-rslR cells
    Concentration: 0-8 μM
    Incubation Time: 24 hours
    Result: Inhibited GPX4 expression, increased p62 and Nrf2 levels, and decreased Keap1 levels.
    In Vivo

    RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with trigonelline in mice bearing HN3R cells.

    Animal Model: Ten-week-old athymic BALB/c male nude mice (nu/nu) bearing HN3R cells[1]
    Dosage: 100 mg/kg in combination with trigonelline (50 mg/kg)
    Administration: Intratumorally twice per week for 20 days
    Result: Significantly reduced the volume of tumor combined with trigonelline in mice.
    Molecular Weight

    440.88

    Formula

    C₂₃H₂₁ClN₂O₅

    CAS No.

    1219810-16-8

    SMILES

    O=C([[email protected]]1CC2=C([[email protected]](C3=CC=C(C(OC)=O)C=C3)N1C(CCl)=O)NC4=C2C=CC=C4)OC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 153.85 mg/mL (348.96 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2682 mL 11.3410 mL 22.6819 mL
    5 mM 0.4536 mL 2.2682 mL 4.5364 mL
    10 mM 0.2268 mL 1.1341 mL 2.2682 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 5 mg/mL (11.34 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 5 mg/mL (11.34 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 5 mg/mL (11.34 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    RSL3(1S,3R)-RSL3RSL 3RSL-3Glutathione PeroxidaseFerroptosisInhibitorinhibitorinhibit

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    Product Name:
    RSL3
    Cat. No.:
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