1. Metabolic Enzyme/Protease
  2. Glutathione Peroxidase
  3. (1S,3R)-RSL3

(1S,3R)-RSL3 

Cat. No.: HY-100218A Purity: 99.87%
Handling Instructions

(1S,3R)-RSL3 is an inhibitor of glutathione peroxidase 4 (GPX4), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. (1S,3R)-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.

(1S,3R)-RSL3 Chemical Structure

(1S,3R)-RSL3 Chemical Structure

CAS No. : 1219810-16-8

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10 mM * 1 mL in DMSO USD 87 In-stock
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25 mg USD 330 In-stock
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100 mg USD 990 In-stock
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Based on 6 publication(s) in Google Scholar

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Description

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

IC50 & Target

Glutathione peroxidase 4[1]

In Vitro

(1S,3R)-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].
(1S,3R)-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

(1S,3R)-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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (226.82 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: ≥ 2.5 mg/mL (5.67 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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(1S,3R)-RSL3
Cat. No.:
HY-100218A
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