Imidazole ketone erastin (Synonyms: IKE)

Name: Imidazole ketone erastin
Brand: MedChemExpress
SKU: HY-114481
Rating: 5.0 (50 reviews)

Cat. No.: HY-114481 Purity: 99.77%: Data Sheet
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Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system x_c^- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.

For research use only. We do not sell to patients.

CAS No. : 1801530-11-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 50 publication(s) in Google Scholar

Other Forms of Imidazole ketone erastin:

Erastin In-stock

50 Publications Citing Use of MCE Imidazole ketone erastin

Cell Proliferation/Viability Assay

Histological Imaging/Staining

In Vivo Efficacy Study

: Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Aug 7;85(15):2973-2987.e6. [Abstract]; KU1919 cells were treated with DMSO or 5 μM tazemetostat for 24 hours, followed by 24-hour treatment with 5 μM imidazole ketone erastin.

: Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Aug 7;85(15):2973-2987.e6. [Abstract]; Imidazole ketone erastin (50 mg/kg, i.p. injection) was administered. Growth curves of tumors derived from KU1919 cells in xenograft mouse models were recorded.

: Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Aug 7;85(15):2973-2987.e6. [Abstract]; Imidazole ketone erastin (50 mg/kg, i.p. injection) was administered. Representative H&E and immunostaining images of Ki67, ACSL4, ETNK1, PTGS2, 4-HNE and SO2/3-PRDX3 were shown from sections of xenograft tumors with indicated treatment. Scale bars: 40 μm.

: Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 21;15(1):2531. [Abstract]; Cell viability of A549 sgNC re-expressed with vector, sgGAS41 cells re-expressed with vector, GAS41 WT, GAS41 W93A mutant, or GAS41 L211A mutants was treated with imidazole ketone erastin (3 μM, right panel) for 24 h.

: Imidazole ketone erastin purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Apr;3(4):471-485. [Abstract]; Imidazole ketone erastin and PPG were used at a concentration of 45 mg/kg/d through intraperitoneal injection. Tumor weight after combination treatment with IKE and PPG was measured.

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Biological Activity
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References
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Description

IC₅₀ & Target

System X_c^-, ferroptosis^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CCF-STTG1	IC₅₀	30 nM Compound: IKE	Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry	[PMID: 26231156]
DOHH-2	IC₅₀	0.014 μM Compound: 6; IKE	Anticancer activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Anticancer activity against human DOHH-2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 36332549]
HT-1080	GI₅₀	314 nM Compound: IKE	Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay Growth inhibition of human HT1080 cells after 48 hrs by alamar blue assay	[PMID: 26231156]
SU-DHL-16	IC₅₀	0.012 μM Compound: 6; IKE	Anticancer activity against human SU-DHL-16 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Anticancer activity against human SU-DHL-16 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 36332549]
SU-DHL-2	IC₅₀	0.021 μM Compound: 6; IKE	Anticancer activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Anticancer activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 36332549]
SU-DHL-5	IC₅₀	0.001 μM Compound: 6; IKE	Anticancer activity against human SU-DHL-5 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Anticancer activity against human SU-DHL-5 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 36332549]
SU-DHL-6	IC₅₀	0.001 μM Compound: 6; IKE	Anticancer activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Anticancer activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 36332549]
SU-DHL10	IC₅₀	0.004 μM Compound: 6; IKE	Anticancer activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Anticancer activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 36332549]

In Vitro

Imidazole ketone erastin (IKE) (0.1 nM-100 μM; 24 h) potently reduces diffuse large B cell lymphoma (DLBCL) cell number by lipid peroxidation and ferroptosis^[1].
IKE (1-250 nM; 24 h) depletes reduced glutathione (GSH) in a dose-dependent manner with an IC₅₀ of 34 nM in SUDHL6 cells^[1].
IKE (125-500 nM) increases lipid ROS in a dose-dependent manner in SUDHL-6 cells^[1].
IKE (500 nM; 5-360 min) increases the system x_c component SLC7A11, prostaglandin-endoperoxide synthase 2 (PTGS2), and ChaC glutathione-specific gamma-glutamylcyclotransferase 1 (CHAC1) expression in SUDHL-6 cells^[1].
IKE (500 nM and 1 μM) changes the relative abundance of 62 lipid species including lysophosphatidylcholines (LPC), phosphatidylcholines (PC), phosphatidylethanolamines (PE), and triglycerides (TAGs) in SUDHL6 cells^[1].
IKE (500 nM) activates de novo lipid biosynthesis pathways, phospholipid remodeling pathways, and arachidonic acid oxidation pathways in SUDHL6 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

IKE (23-40 mg/kg; i.p. once daily for 13 d) inhibits tumor growth in mice^[1].
IKE (50 mg/kg; a single i.p) depletes GSH significantly starting from 4 h, and increases in the relative abundance of free fatty acids, phospholipids, and diacylglycerols (DAG) in mice^[1].
IKE (50 mg/kg) exhibits half-life (1.82, 1.31, and 0.96 h) and C_max (19515, 11384, and 5203 ng/mL) following different administration (i.p., i.v., and p.o. respectively) in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male NCG mice bearing SUDHL6 subcutaneous xenografts^[1]
Dosage:	23, 40 mg/kg
Administration:	I.p. injection once daily for 13 days
Result:	Caused a significant decrease in tumor growth starting from day 9. Had a weight loss starting from day 9.

Animal Model:	NOD/SCID mice (12 weeks old; ~28 g weight)^[1]
Dosage:	50 mg/kg (Pharmacokinetic Analysis)
Administration:	A single i.p., i.v., and p.o. administration
Result:	I.p.: T_1/2=1.82 h, C_max=19515 ng/mL. I.v.: T_1/2=1.31 h, C_max=11384 ng/mL. P.o.: T_1/2=0.96 h, C_max=5203 ng/mL.

Clinical Trial

Molecular Weight

655.14

Formula

C₃₅H₃₅ClN₆O₅

CAS No.

1801530-11-9

Appearance

Solid

Color

White to yellow

SMILES

O=C1N(C2=CC(C(CN3C=CN=C3)=O)=CC=C2OC(C)C)C(CN4CCN(C(COC5=CC=C(Cl)C=C5)=O)CC4)=NC6=CC=CC=C61

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (152.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5264 mL	7.6320 mL	15.2639 mL
5 mM	0.3053 mL	1.5264 mL	3.0528 mL
10 mM	0.1526 mL	0.7632 mL	1.5264 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (283 KB) SDS (396 KB)

COA (257 KB) HNMR (144 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang Y, et al. Imidazole Ketone Erastin Induces Ferroptosis and Slows Tumor Growth in a Mouse Lymphoma Model. Cell Chem Biol. 2019 Jan 31. pii: S2451-9456(19)30030-3. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5264 mL	7.6320 mL	15.2639 mL	38.1598 mL
	5 mM	0.3053 mL	1.5264 mL	3.0528 mL	7.6320 mL
	10 mM	0.1526 mL	0.7632 mL	1.5264 mL	3.8160 mL
	15 mM	0.1018 mL	0.5088 mL	1.0176 mL	2.5440 mL
	20 mM	0.0763 mL	0.3816 mL	0.7632 mL	1.9080 mL
	25 mM	0.0611 mL	0.3053 mL	0.6106 mL	1.5264 mL
	30 mM	0.0509 mL	0.2544 mL	0.5088 mL	1.2720 mL
	40 mM	0.0382 mL	0.1908 mL	0.3816 mL	0.9540 mL
	50 mM	0.0305 mL	0.1526 mL	0.3053 mL	0.7632 mL
	60 mM	0.0254 mL	0.1272 mL	0.2544 mL	0.6360 mL
	80 mM	0.0191 mL	0.0954 mL	0.1908 mL	0.4770 mL
	100 mM	0.0153 mL	0.0763 mL	0.1526 mL	0.3816 mL

Imidazole ketone erastin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Imidazole ketone erastin1801530-11-9IKEFerroptosiscystineglutamateantiportersystemxc-ferroptosisanti-tumorInhibitorinhibitorinhibit

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Imidazole ketone erastin (Synonyms: IKE)

Customer Review

Other Forms of Imidazole ketone erastin:

Imidazole ketone erastin Related Antibodies

50 Publications Citing Use of MCE Imidazole ketone erastin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Imidazole ketone erastin Related Antibodies

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Complete Stock Solution Preparation Table

Imidazole ketone erastin Related Classifications

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