Home DNA Damage/DNA Repair OGG1 inhibitor TH5487 For research use only.

TH5487

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

TH5487 Chemical Structure

TH5487 Chemical Structure

CAS No. 2304947-71-3

Purity & Quality Control

TH5487 Related Products

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

--
In Vivo
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]
Animal Research Animal Models mice (50% female and 50% male) of which lungs are TNFα-challenged intranasally (20 ng/ml)
Dosages 30 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 541.18 Formula

C19H18BrIN4O2
CAS No. 2304947-71-3 SDF --
Smiles C1CN(CCC1N2C3=C(C(=CC=C3)Br)NC2=O)C(=O)NC4=CC=C(C=C4)I
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 10 mg/mL ( (18.47 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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