TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.
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]
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]
[1] Visnes T, et al.Science. 2018 Nov 16;362(6416):834-839.