TH5487

For research use only.

Catalog No.S8913

TH5487 Chemical Structure

Molecular Weight(MW): 541.18

TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.

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Biological Activity

Description TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.
Targets
OGG1 [1]
(Cell-free assay)
342 nM
In vitro

TH5487 increases the melting temperature of OGG1 in human cells.TH5487 impaires repair of genomic 8-oxoG induced by KBrO3.TH5487 preventes OGG1 binding to its genomic substrate in living cells.[1]

In vivo

To assess whether TH5487 could down-regulate chemotactic (C-C and C-X-C) mediators in vivo, we challenge mouse lungs with TNFα and profile the gene expression of proinflammatory mediators. TH5487 is efficacious in vivo, suggesting that the compound could be used for the treatment of inflammatory conditions. [1]

Protocol

Cell Research:

[1]

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  • Cell lines: HEK 293T cells Wild-type, HEK 293T cells OGG1-KO, MLE12, hSAECs
  • Concentrations: 5 μM
  • Incubation Time: 1 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: mice (50% female and 50% male) of which lungs are TNFα-challenged intranasally (20 ng/ml)
  • Dosages: 30 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (18.47 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 541.18
Formula

C19H18BrIN4O2

CAS No. 2304947-71-3
Storage powder
in solvent
Synonyms N/A

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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