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Imidazole ketone erastin

Cat. No. M10244
Imidazole ketone erastin Structure
Synonym:

Ferroptosis inducer IKE; PUN-30119

Size Price Availability Quantity
5mg USD 200.7  USD223 In stock
10mg USD 324  USD360 In stock
25mg USD 576  USD640 In stock
50mg USD 882  USD980 In stock
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Quality Control
Biological Activity

Imidazole ketone erastin (IKE) is an inducer of ferroptosis, and it is also a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system Xc-. Dramatic improvement of the half-maximal inhibitory constants for system xc− inhibition was observed for IKE (IC50 = 30 nM), compared to erastin and PE. In a diffuse large B cell lymphoma (DLBCL) xenograft model, IKE exerted an antitumor effect by inhibiting system xc-, leading to glutathione depletion, lipid peroxidation, and the induction of ferroptosis biomarkers.

Protocol
Cell Experiment
Cell lines DLBCL cell line
Preparation method DLBCL cells are plated at 10,000 cells per well in white 384-well plates (32 μL per well) in technical duplicates and incubated overnight. The cells are then treated with 8 μL medium containing a two-fold dilution series of vehicle (DMSO), IKE (starting from 100 μM) with or without Fer-1 (starting from 200 μM). After 24 h incubation, 40 μL of 50% CellTiter-Glo / 50% cell culture medium is added to each well and incubated at room temperature with shaking for 15 min. Luminescence is measured. All cell viability data are normalized to the DMSO vehicle condition. Experiments are performed three independent times with different passages for each cell line. From these data, dose-response curves and IC50 values are computed.
Concentrations 0-100 μM
Incubation time 24 h
Animal Experiment
Animal models Non-obese diabetic/ severe combined immunodeficiency (NOD/SCID) mice
Formulation dissolved in 5% DMSO/95% HBSS at pH 4 solution
Dosages 50 mg/kg, 17 mg/kg
Administration IP and PO and IV
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 655.14
Formula C35H35ClN6O5
CAS Number 1801530-11-9
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model
Yan Zhang, et al. Cell Chem Biol. 2019 May 16;26(5):623-633.e9. PMID: 30799221.

Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility
Marie-Helene Larraufie, et al. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4787-4792. PMID: 26231156.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Imidazole ketone erastin, Ferroptosis inducer IKE; PUN-30119 supplier, Ferroptosis, inhibitors

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