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TH5487

Chemical Structure : TH5487

CAS No.: 2304947-71-3

TH5487 (TH-5487)

Catalog No.: PC-35806Not For Human Use, Lab Use Only.

TH5487 (TH-5487, TH 5487) is a potent, selective, active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM, prevents OGG1 from binding to its DNA substrate.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TH5487 (TH-5487, TH 5487) is a potent, selective, active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM, prevents OGG1 from binding to its DNA substrate.
TH5487 does not affect the activity of other DNA glycosylases or various Nudix hydrolases and diphosphatase, also not intercalate DNA.
TH5487 decreases binding of OGG1 to promoters in chromatin, engages OGG1 in cells, inhibits DNA repair, and alters OGG1 chromatin dynamics.
TH5487 specifically inhibit OGG1-dependent proinflammatory gene expression, decreases CXCL1 expression by >50% in wild-type but not in OGG1-knockout cells at 5 uM, inhibits TNFα-induced expression of TNF in hSAECs.
TH5487 suppresses proinflammatory gene expression and lung inflammation in mice (30 mg/kg, i.p.).

Physicochemical Properties

M.Wt 541.187
Formula C19H18BrIN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(4-bromo-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)-N-(4-iodophenyl)piperidine-1-carboxamide

References

1. Visnes T, et al. Science. 2018 Nov 16;362(6416):834-839.

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