TH5487

Catalog No.S8913

For research use only.

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

TH5487 Chemical Structure

CAS No. 2304947-71-3

Selleck's TH5487 has been cited by 1 Publication

Purity & Quality Control

Choose Selective OGG1 Inhibitors

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 (from reference)

Cell Research:

[1]

  • 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]

  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1N2C3=C(C(=CC=C3)Br)NC2=O)C(=O)NC4=CC=C(C=C4)I

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

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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

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