TH5487

产品编号: DC23145 Featured
TH5487
结构式
2304947-71-3
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中国地区超过5000个高品质化合物库存
应用领域
TH5487 是一种有效的 8-氧鸟嘌呤 DNA 糖基化酶1 (OGG1) 抑制剂,IC50 为342 nM,TH5487 阻止 OGG1 识别其 DNA 底物,抑制 DNA 修复和修饰 OGG1 染色质动力学,从而抑制促炎基因。
Cas No.: 2304947-71-3
名称: 4-(4-bromo-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)-N-(4-iodophenyl)piperidine-1-carboxamide
别名: TH5487,TH-5487,TH 5487
SMILES: O=C(NC1=CC=C(I)C=C1)N(CC2)CCC2N(C3=CC=CC(Br)=C3N4)C4=O
分子式: C19H18BrIn4O2
分子量: 541.187
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.).
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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