IKE(Imidazole ketone erastin)

Catalog No.S8877 Batch:S887704

Technical Data

Formula	C₃₅H₃₅ClN₆O₅
Molecular Weight	655.14	CAS No.	1801530-11-9
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (152.63 mM)
		Ethanol	100 mg/mL (152.63 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.

Targets

Ferroptosis ^[1]

system xc– ^[1]

In vitro

Imidazole ketone erastin (IKE) is an erastin analog with nanomolar potency, high metabolic stability, and intermediate water solubility. Its treatment potently reduces DLBCL cell number^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines DLBCL cell line Concentrations 0-100 μM Incubation Time 24 h 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.
Animal Study:^{^[1]}	Animal Models Non-obese diabetic/ severe combined immunodeficiency (NOD/SCID) mice Dosages 50 mg/kg Administration IP, IV and oral administration

Cell Assay:^{^[1]}

Cell lines
DLBCL cell line
Concentrations
0-100 μM
Incubation Time
24 h
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.

Animal Study:^{^[1]}

Animal Models
Non-obese diabetic/ severe combined immunodeficiency (NOD/SCID) mice
Dosages
50 mg/kg
Administration
IP, IV and oral administration

References

[1] Zhang Y, et al. Cell Chem Biol. 2019, 26(5):623-633.e9.

Selleck's IKE(Imidazole ketone erastin) has been cited by 25 publications

Meningioma achieves malignancy and erastin-induced ferroptosis resistance through FOXM1-AURKA-NRF2 axis [ Redox Biol, 2024, 72:103137]	PubMed: 38642502
Augmented ERO1α upon mTORC1 activation induces ferroptosis resistance and tumor progression via upregulation of SLC7A11 [ J Exp Clin Cancer Res, 2024, 43(1):112]	PubMed: 38610018
CYLD regulates cell ferroptosis through Hippo/YAP signaling in prostate cancer progression [ Cell Death Dis, 2024, 15(1):79]	PubMed: 38246916
Mutational signature-based identification of DNA repair deficient gastroesophageal adenocarcinomas for therapeutic targeting [ NPJ Precis Oncol, 2024, 8(1):87]	PubMed: 38589664
Phospholipase PLA2G7 is complementary to GPX4 in mitigating punicic-acid-induced ferroptosis in prostate cancer cells [ iScience, 2024, 27(5):109774]	PubMed: 38711443
Intermittent dietary methionine deprivation facilitates tumoral ferroptosis and synergizes with checkpoint blockade [ Nat Commun, 2023, 14(1):4758]	PubMed: 37553341
Intermittent dietary methionine deprivation facilitates tumoral ferroptosis and synergizes with checkpoint blockade [ Nat Commun, 2023, 14(1):4758]	PubMed: 37553341
RB1-deficient prostate tumor growth and metastasis are vulnerable to ferroptosis induction via the E2F/ACSL4 axis [ J Clin Invest, 2023, 133(10)e166647]	PubMed: 36928314
RB1-deficient prostate tumor growth and metastasis are vulnerable to ferroptosis induction via the E2F/ACSL4 axis [ J Clin Invest, 2023, 133(10)e166647]	PubMed: 36928314
Targeting N-glycosylation of 4F2hc mediated by glycosyltransferase B3GNT3 sensitizes ferroptosis of pancreatic ductal adenocarcinoma [ Cell Death Differ, 2023, 30(8):1988-2004]	PubMed: 37479744

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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