1. Apoptosis
  2. Ferroptosis
  3. Imidazole ketone erastin

Imidazole ketone erastin (Synonyms: IKE)

Cat. No.: HY-114481 Purity: 99.67%
Handling Instructions

Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.

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

Imidazole ketone erastin Chemical Structure

Imidazole ketone erastin Chemical Structure

CAS No. : 1801530-11-9

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10 mM * 1 mL in DMSO USD 360 In-stock
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5 mg USD 250 In-stock
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10 mg USD 350 In-stock
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50 mg USD 1100 In-stock
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100 mg USD 1800 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Imidazole ketone erastin:

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  • Biological Activity

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Description

Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc- and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity[1].

IC50 & Target

System Xc-, ferroptosis[1]

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 xc 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].

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 Cmax (19515, 11384, and 5203 ng/mL) following different administration (i.p., i.v., and p.o. respectively) in mice[1].

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.: T1/2=1.82 h, Cmax=19515 ng/mL.
I.v.: T1/2=1.31 h, Cmax=11384 ng/mL.
P.o.: T1/2=0.96 h, Cmax=5203 ng/mL.
Molecular Weight

655.14

Formula

C₃₅H₃₅ClN₆O₅

CAS No.

1801530-11-9

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 : ≥ 125 mg/mL (190.80 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.17 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.67%

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Keywords:

Imidazole ketone erastinIKEFerroptosiscystineglutamateantiportersystemxc-ferroptosisanti-tumorInhibitorinhibitorinhibit

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Imidazole ketone erastin
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