2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
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; does not affect the activity of other DNA glycosylases or various Nudix hydrolases and diphosphatase, also not intercalate DNA; decreases binding of OGG1 to promoters in chromatin, engages OGG1 in cells, inhibits DNA repair, and alters OGG1 chromatin dynamics; 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; suppresses proinflammatory gene expression and lung inflammation in mice (30 mg/kg, i.p.).
