Imidazole ketone erastin (PUN30119)

For research use only.

Catalog No.S8877 Synonyms: IKE

8 publications

Imidazole ketone erastin (PUN30119) Chemical Structure

CAS No. 1801530-11-9

Imidazole ketone erastin (PUN30119, IKE) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis.

Selleck's Imidazole ketone erastin (PUN30119) has been cited by 8 publications

Purity & Quality Control

Choose Selective Ferroptosis Inhibitors

Biological Activity

Description Imidazole ketone erastin (PUN30119, IKE) 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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BJeLR MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmK2OFghcHK| MWjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDSRXMuTzF{VjDveoVz\XiycnXzd4lv\yCESnXMVkBk\WyuczDh[pRmeiB2ODDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVAhRSByLkCwN{DPxE1w NETsXm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKzNVE2Pid-Mk[yN|EyPTZ:L3G+
CCF-STTG1 NUfy[4lzTnWwY4Tpc44h[XO|YYm= M1LVXFIhcHK| Ml\jTY5pcWKrdHnvckBw\iC[Y4SgbY4hcHWvYX6gR2NHNVOWVFexJINmdGy|IHHzd4V{e2WmIHHzJIdtfXSjbXH0[UBz\WynYYPlJIFnfGW{IEKgbJJ{KGK7IH\seY9zd22ndIL5MEBKSzVyIE2gNE4xOyEQvF2u MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ|MUG1Okc,OjZ{M{GxOVY9N2F-
HT1080 MmnIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFXFOWM1QCCqcoO= MnPsS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTHQyODhyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBidGGvYYKgZox2\SCjc4PhfUwhT0l3MDC9JFAvOzF2IN88UU4> NIO1U3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKzNVE2Pid-Mk[yN|EyPTZ:L3G+
DRD NFO5WZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVO0PEBpenN? MXfHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDSRXMuTzF{VjDveoVz\XiycnXzd4lv\yCGUlSgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6 NECwTXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKzNVE2Pid-Mk[yN|EyPTZ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 30799221     


DLBCL cell line sensitivity was measured by incubating cells with a 2-fold series dilution of IKE (starting from 100 mM) for 24 h followed by a CellTiter-Glo luminescent cell viability test. LY8, DOHH2, SUDHL5, SUDHL2, SUDHL6, SUDHL10, and SUDHL16 were classified as sensitive cell lines (red). HBL1, SUDHL9, WSU-NHL, SUDHL8, RIVA, and KARPAS422 were classified as moderately resistant cell lines (black). SUDHL7, U937, A3/KAW, LY7, and U2932 were classified as resistant cell lines (blue).

30799221

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (152.63 mM)
Water Insoluble
Ethanol ''33 mg/mL

* 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.

Chemical Information

Molecular Weight 655.14
Formula

C35H35ClN6O5

CAS No. 1801530-11-9
Storage powder
in solvent
Synonyms IKE
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01555008 Completed Drug: LX4211|Drug: LX4211 Placebo Type 2 Diabetes Mellitus|Renal Impairment Lexicon Pharmaceuticals March 2012 Phase 1
NCT04545450 Completed Drug: dutasteride 5 mg/day|Drug: Testosterone Undecanoate Transgenderism|Hypogonadism Unita Complessa di Ostetricia e Ginecologia November 4 2008 Phase 3

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID