Biological Activity

TH5487 is a selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 (5 μM; 1 hour) decreases TNFα- and LPS-induced proinflammatory gene expression to near pretreatment levels. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes.

In vivo, TH5487 (prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours) decreases TNFα or LPS induced the robust recruitment of neutrophils to the airways, and reduces the pulmonary neutrophil count in a time-dependent manner.

Chemical Information

Molecular Weight	541.18
Formula	C19H18BrIN4O2
CAS Number	2304947-71-3
Solubility (25°C)	DMSO ≥ 13 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Visnes T, et al. Science. Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation.