Liproxstatin-1

For research use only.

Catalog No.S7699

72 publications

Liproxstatin-1 Chemical Structure

CAS No. 950455-15-9

Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.

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Selleck's Liproxstatin-1 has been cited by 72 publications

Purity & Quality Control

Choose Selective Ferroptosis Inhibitors

Biological Activity

Description Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM.
Targets
ferroptosis [1]
(Cell-free assay)
22 nM
In vitro

Liproxstatin-1 is able to inhibit ferroptosis in the low nanomolar range and inhibit the growth of Gpx4−/−cells with IC50 of 22 nM. Liproxstatin-1 (50 nM) completely prevents lipid peroxidation in Gpx4−/−cells. Liproxstatin-1 (200 nM) protects against FINs, such as BSO (10 µM), erastin (1 µM) and RSL3 (0.5 µM), in a dose dependent manner, whereas it fails to rescue cell death induced by staurosporine (0.2 µM) and H2O2 (200 µM).[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MRC-5 lung fibroblast cells M{\6XGRPTEl8IFP5eI91d3irY3n0fUBi\2GrboP0JIh2dWGwIF3SR{02KGy3bneg[oljem:kbHHzeEBk\WyuczygTWM2OCB;IEmuNVQh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNFk1PzVyLze+R4hGVUKOPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
GPX4 / β-actin; 

PubMed: 33602915     


IEC6 cells were co-cultured with 100 μM compound 5 or 50 nM liproxstatin-1 for 4 h (ROS and GSH experiments) or 24 h (survival experiment). C) WB images showed expression of GPX4 protein in IEC6 cells.

GRP78 / CHOP / Actin; 

PubMed: 29383150     


The combinatorial treatment of ferroptotic agent and TRAIL promotes apoptosis via ER stress, but not lipid peroxidation in HCT116 cells. Cells were treated with 50 μM ART for 24 h in the absence/presence of DFO (100 μM), ferrostatin-1 (Fer-1, 10 μM), or liproxstatin-1 (Lip-1, 2 μM).

GRP78 / CHOP / Actin; 

PubMed: 29383150     


The combinatorial treatment of ferroptotic agent and TRAIL promotes apoptosis via ER stress, but not lipid peroxidation in HCT116 cells. Cells were treated with 50 μM Erastin for 24 h in the absence/presence of DFO (100 μM), ferrostatin-1 (Fer-1, 10 μM), or liproxstatin-1 (Lip-1, 2 μM).

NeuN / Syn / SNAP / GFAP / Actin / Tubulin; 

PubMed: 28212525     


Western blots showing attenuated neurodegeneration (NeuN, Synaptophysin, SNAP25) and neuroinflammation (GFAP) in HC of Gpx4BIKO-VED mice treated with the ferroptosis inhibitor liproxstatin-1 compared to Gpx4BIKO-VED mice treated with vehicle (DMSO) at 1 week post TAM treatment (n=5 for all groups).

β-actin / COX2 / GPx4; 

PubMed: 30737476     


Liproxstatin-1 inhibits lipid peroxidation and cell death in vitro. Caco-2 cells were pretreated with liproxstatin-1 (200 nM) for 12 h before being subjected to H/R (H, 12 h of hypoxia; R, 2 h of reoxygenation). All samples were collected after H/R. a GPx4 and COX2 expression in cells were detected by western blotting (n = 3).

β-actin / COX2 / GPx4; 

PubMed: 30737476     


Liproxstatin-1 ameliorates ferroptosis and intestinal injury in vivo. Mice were treated with liproxstatin-1 (10 mg/kg) by intraperitoneal injection 1 h before ischemia and then subjected to ischemia/reperfusion (I, 45 min of ischemia; R, 30 min of reperfusion) or sham surgery (sham). All samples were collected after I/R. a GPx4 and COX2 levels were assessed by western blotting (n = 3).

COX2 / GPx4 / GAPDH; 

PubMed: 33889074     


Liproxstatin-1 inhibits ferroptosis after stroke. (A) The protein levels of COX2 and GPx4 in peri-infarct region of sham group, MCAO group, sham + Lip group and MCAO + Lip group at 24 h after cerebral ischemic reperfusion, respectively.

33602915 29383150 28212525 30737476 33889074
Growth inhibition assay
Cell viability; 

PubMed: 31641008     


(B-C) Two ferroptosis inhibitors rescued cystine deprivation-induced cell death. TOV-21G cells were seeded in 10% (20 μM of cystine) or 20% (40 μM of cystine) of full DMEM media supplied with or without either 200 nM liproxstatin-1 (B) or 2 μM ferrostatin-1.

31641008
Immunofluorescence
mitochondrial Fe2+; 

PubMed: 33343803     


Fluorescence microscopic analysis for detecting mitochondrial Fe2+ and lipid peroxidation in neomycin-damaged HEI-OC1 cells. Representative images of Mito-FerroGreen staining in the (a) control, (b) Lip-1, (c) neomycin (Neo), and (d) Lip-1+neomycin cotreatment (Lip-1+Neo); scale bars indicate 10 μm.

NeuN / ACSL4; 

PubMed: 33314758     


(F) Immunofluorescence analysis performed using antibodies specific for ACSL4 (red), a neuronal marker (green), and DAPI nuclear stain (blue). Scale bar = 100 μm. (G) Quantification analysis of the relative fluorescence intensity of ACSL4. **p < 0.0001 vs. Sham group; ## p = 0.5136, @@ p = 0.8177 vs. SAH + Vehicle group; results analyzed using unpaired t‐test, n = 6. All data are shown as mean ± SEM. Mean values of the Sham group were normalized to 1.0.

β-actin / COX2 / GPx4; 

PubMed: 30737476     


Cell lipid peroxidation were detected by BODIPY 581/591 C11 staining using fluorescence microscopy (scale bar = 100 μm) and 12-HETE, 15-HETE, and LPO assay kits (n = 6).

33343803 33314758 30737476
In vivo Liproxstatin-1 remarkably extends survival compared with the vehicle-treated group, delays ferroptosis in tubular cells, and mitigates tissue injury in ischaemia/reperfusion-induced liver injury. [1]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: Gpx4−/−cells
  • Concentrations: ~200 nM
  • Incubation Time: ~72 h
  • Method:

    Cell viability is assessed at different time points after treatment using AquaBluer according to the manufacturer’s recommendations. Alternatively, cell death is also quantified by measuring released lactate dehydrogenase activity using the cytotoxicity detection kit (LDH).


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: GreERT2; Gpx4fI/fI mice
  • Dosages: 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (199.5 mM)
Water Insoluble
Ethanol '21 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/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 340.85
Formula

C19H21ClN4

CAS No. 950455-15-9
Storage powder
in solvent
Synonyms N/A
Smiles C1CNCCC12C(=NCC3=CC(=CC=C3)Cl)NC4=CC=CC=C4N2

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID