|4-(4-溴-2-氧代-2,3-二氢-1H-苯并[d]咪唑-1-基)-N-(4-碘苯基)哌啶-1-甲酰胺|CsnPharm

CAS No.: 2304947-71-3

TH5487 is selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with IC50 of 342 nM.

规格	价格	促销价格	库存	数量

400-920-2911

加入购物车大规格询价

产品咨询

400-920-2911

纯度 & 质量文件批次:

生物活性

描述The onset of inflammation is associated with reactive oxygen species and oxidative damage to macromolecules like 7,8-dihydro-8-oxoguanine (8-oxoG) in DNA. 8-Oxoguanine DNA glycosylase 1 (OGG1) binds with high affinity to 8-oxoG in double-stranded DNA to initiate DNA base excision repair. TH5487, a potent and selective OGG1 inhibitor with an IC₅₀ of 342 nM, hampers OGG1 binding to and repair of 8-oxoG. The amount of OGG1-DNA complexes decreased in a dose-dependent manner upon addition of TH5487, demonstrating that TH5487 precludes OGG1 from binding oxidized DNA in vitro. TH5487 (10 μM) increased the melting temperature of OGG1 in Jurkat A3 cells, demonstrating that TH5487 protected it from thermal denaturation. Further, treatment with 5 μM TH5487 decreased CXCL1 (a proinflammatory gene) expression by >50% in human embryonic kidney (HEK) 293T cells suggesting TH5487 can specifically inhibit OGG1-dependent proinflammatory gene expression. Crucially, TH5487 decreased TNFα- and LPS-induced gene expression in diploid human small-airway epithelial cells (hSAECs) as well. In vivo, TNFα (20 ng/ml) robustly induced the expression of pulmonary proinflammatory genes in mice, but a prophylactic injection of TH5487 (30 mg/kg) decreased the expression levels^[1].
参考文献

实验方案

技术信息

CAS号

2304947-71-3

储存条件

分子式

C19H18BrIN4O2

运输

蓝冰

分子量

541.18

别名

溶解度

DMSO	25.0 mg/mL (46.2 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

请登录您的专属账户