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Submit ReviewTH 5487
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)
Biological Activity for TH 5487
TH 5487 is a 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 for TH 5487
| 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 for TH 5487
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.12 | 100 |
Preparing Stock Solutions for TH 5487
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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Product Datasheets for TH 5487
References for TH 5487
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
2 Citations for TH 5487
Citations are publications that use Tocris products. Selected citations for TH 5487 include:
Eric L et al (2022) Oxidative DNA Damage and Cisplatin Neurotoxicity Is Exacerbated by Inhibition of OGG1 Glycosylase Activity and APE1 Endonuclease Activity in Sensory Neurons. Int J Mol Sci 23 PMID: 35163831
Janice et al (2022) Interplay between H3K36me3, methyltransferase SETD2, and mismatch recognition protein MutSα facilitates processing of oxidative DNA damage in human cells. J Biol Chem 298 102102 PMID: 35667440
Do you know of a great paper that uses TH 5487 from Tocris? Please let us know.
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