TH 5487

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Cat.No. 6749 - TH 5487 | C19H18BrIN4O2 | CAS No. 2304947-71-3
Description: Selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor
Chemical Name: 4-(4-Bromo-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-N-(4-iodophenyl)-1-piperidinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

Selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor (IC50 = 342 nM). Selective for OGG1 over other base excision repair enzymes. Inhibits OGG1 binding to 8-oxoG in DNA and suppresses proinflammatory gene expression in TNF-α stimulated lung epithelial cells in vitro. Also inhibits proinflamatory gene expression and neutrophil recruitment in TNF-α-challenged mouse lungs in vivo.

Licensing Information

Sold under license from Thomas Helleday's Foundation for Medical Research and Oxcia AB.

Technical Data

M. Wt 541.18
Formula C19H18BrIN4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2304947-71-3
PubChem ID 137321164
InChI Key FZLKVWWPFOLPKF-UHFFFAOYSA-N
Smiles O=C(NC1=CC=C(I)C=C1)N(CC2)CCC2N(C3=CC=CC(Br)=C3N4)C4=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 54.12 100

Preparing Stock Solutions

The following data is based on the product molecular weight 541.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.85 mL 9.24 mL 18.48 mL
5 mM 0.37 mL 1.85 mL 3.7 mL
10 mM 0.18 mL 0.92 mL 1.85 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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References

References are publications that support the biological activity of the product.

Visnes et al (2018) Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation. Science 362 834 PMID: 30442810


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Keywords: TH 5487, TH 5487 supplier, TH5487, OGG1, inhibitors, inhibits, selective, 8-oxoguanine, DNA, glycosylase, 1, repair, enzymes, anti-inflammatory, Glycosylases, 6749, Tocris Bioscience

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