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IKE(Imidazole ketone erastin)

Name: IKE(Imidazole ketone erastin)
Brand: Selleck Chemicals
SKU: S8877
Rating: 5 (26 reviews)

Synonyms: PUN30119

Catalog No.S8877 Purity:99.51%

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

IKE(Imidazole ketone erastin) Chemical Structure

CAS No. 1801530-11-9

Purity & Quality Control

Batch: Purity: 99.51%

99.51

Products often used together with IKE(Imidazole ketone erastin)

Rapamycin

Imidazole ketone erastin and Rapamycin induce cell death in acute lymphoblastic leukemia (ALL) cell lines Jurkat/CCRF-CEM/CEM/C1/Nalm6/Sup-B15/THP-1/HL-60.

Zhu T, et al. Front Cell Dev Biol. 2021 Nov 15;9:740884.

IKE(Imidazole ketone erastin) Related Products

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Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
BJeLR	Growth inhibition assay	48 hrs	Growth inhibition of human RAS-G12V overexpressing BJeLR cells after 48 hrs by alamar blue assay, IC50 = 0.003 μM.	26231156
CCF-STTG1	Function assay	2 hrs	Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry, IC50 = 0.03 μM.	26231156
HT1080	Growth inhibition assay	48 hrs	Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay, GI50 = 0.314 μM.	26231156
DRD	Growth inhibition assay	48 hrs	Growth inhibition of human RAS-G12V overexpressing DRD cells after 48 hrs by alamar blue assay	26231156
Click to View More Cell Line Experimental Data

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
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].
Cell Research	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Growth inhibition assay	Cell viability		30799221

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01555008	Completed	Type 2 Diabetes Mellitus\|Renal Impairment	Lexicon Pharmaceuticals	March 2012	Phase 1
NCT04545450	Completed	Transgenderism\|Hypogonadism	Unita Complessa di Ostetricia e Ginecologia	November 4 2008	Phase 3

References

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

Chemical Information & Solubility

Molecular Weight	655.14	Formula	C₃₅H₃₅ClN₆O₅
CAS No.	1801530-11-9	SDF	--
Smiles	CC(C)OC1=C(C=C(C=C1)C(=O)CN2C=CN=C2)N3C(=NC4=CC=CC=C4C3=O)CN5CCN(CC5)C(=O)COC6=CC=C(C=C6)Cl
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (152.63 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (7.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5% DMSO 1 95% Corn oil	0.35mg/ml (0.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 Corn oil	5.0mg/ml (7.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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