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Imidazole Ketone Erastin (Synonyms: IKE)

Catalog No.GC52190

Imidazole Ketone Erastin is a ferroptosis inducer.

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Imidazole Ketone Erastin Chemical Structure

Cas No.: 1801530-11-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$113.00
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2mg
$78.00
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5mg
$147.00
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25mg
$441.00
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100mg
$728.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

DLBCL cells

Preparation Method

DLBCL cells were plated at 10,000 cells per well in white 384-well plates in technical duplicates and incubated overnight. The cells were then treated with 8 µL medium containing a two-fold dilution series of vehicle , Imidazole Ketone Erastin (0.1 nM-100 µM ) with or without Fer-1. After 24 h incubation, 40 µL of 50% Cell Titer-Glo 50% cell culture medium was added to each well and incubated at room temperature with shaking for 15 min.

Reaction Conditions

0.1 nM-100 µM; 24 h

Applications

Imidazole ketone erastin (0.1nM-100µM;24h) potently reduces DLBCL cell number by lipid peroxidation and ferroptosis.

Animal experiment [2]:

Animal models

Male NCG mice

Preparation Method

NCG mice, 6-weeks old, were injected with 10 million SUDHL0-6 cells subcutaneously. The mice were treated after the tumor size reached 100 mm3. Mice were separated randomly into treatment groups and dosed with 23 mg/kg Imidazole Ketone Erastin , 40 mg/kg Imidazole Ketone Erastin , 23 mg/kg Imidazole Ketone Erastin PEG-PLGA nanoparticles , vehicle 1, and vehicle 2 once daily by IP for 14 days.

Dosage form

23, 40 mg/kg/d ; 14 days ; i.p.

Applications

Imidazole Ketone Erastin inhibited tumor growth in a diffuse large B cell lymphoma mouse model, caused a significant decrease in tumor growth and weight loss starting from day 9.

References:

[1] Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019).

Background

Imidazole Ketone Erastin is an effective and metabolically stable system xc- inhibitor and ferroptosis inducer. Ferroptosis is a regulated form of cell death that can be induced by inhibiting the cystine-glutamate antiporter system xc- [1].

In vitro, Imidazole Ketone Erastin (0.1 nM-100 µM; 24 h) effectively reduces the number of DLBCL cells by inducing lipid peroxidation and ferroptosis, with 18 DLBCL cell lines displaying varying sensitivities to the inhibition by Imidazole Ketone Erastin [1]. Imidazole Ketone Erastin (1-250 nM; 24 h) depletes reduced glutathione in a dose-dependent manner, with an IC50 of 34 nM in SUDHL 6 cells, and also increases lipid ROS [1].

In vivo, Imidazole Ketone Erastin (23, 40 mg/kg/d; i.p.) inhibits tumor growth in a mouse model of diffuse large B cell lymphoma, leading to a significant reduction in tumor growth and body weight loss starting from day 9 [1]. Imidazole Ketone Erastin (40 mg/kg; i.p.) administered every other day for 22 days to mice with a model of chronic arthritis significantly alleviates symptoms of synovitis and promotes the rapid resolution of inflammation [2].

References:
[1]Zhang, Y., Tan, H., Daniels, J.D., et al. Imidazole ketone erastin induces ferroptosis and slows tumor growth in a mouse lymphoma model. Cell Chem. Biol. 26(5), 623-633 (2019).
[2] TNF antagonist sensitizes synovial fibroblasts to ferroptotic cell death in collagen-induced arthritis mouse models[J]. Nature Communications[2024-03-08].

Chemical Properties

Cas No. 1801530-11-9 SDF Download SDF
Synonyms IKE
Canonical SMILES O=C1N(C2=CC(C(CN3C=NC=C3)=O)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61
Formula C35H35ClN6O5 M.Wt 655.1
Solubility DMF: 10mg/mL; DMSO: 100mg/mL; DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL Storage Store at -20°C
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

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1 mg 5 mg 10 mg
1 mM 1.5265 mL 7.6324 mL 15.2648 mL
5 mM 0.3053 mL 1.5265 mL 3.053 mL
10 mM 0.1526 mL 0.7632 mL 1.5265 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 ddH2O, mix and clarify.

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

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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