Synonyms: TH-5487
Compound class:
Synthetic organic
Comment: TH5487 is a selective, active-site inhibitor of 8-oxoguanine DNA glycosylase (OGG1) [2]. OGG1 repairs 8-hydroxy-2′-deoxyguanosine (8-oxoG) DNA defects that can be induced by reactive oxygen species (ROS) at sites of inflammation. TH5487 inhibits OGG1-mediated proinflammatory activity in allergic states. In a mouse model of allergic airway inflammation TH5487 reduced NF-κB-mediated expression of proinflammatory cytokines/chemokines and inhibited immune cell recruitment into the lungs with an associated reduction in goblet cell hyperplasia and mucus production [1].
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Bioactivity Comments |
TH5487 increased the melting temperature of OGG1 in human cells thus demonstrating target engagement in living cells [2]. TH5487 inhibits immune cell recruitment in vivo [2]. |
Selectivity at enzymes | ||||||||||||||||||||||||||||||||||
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