产品说明书

TH5487

Print
Chemical Structure| 2304947-71-3 同义名 : -
CAS号 : 2304947-71-3
货号 : A1216731
分子式 : C19H18BrIN4O2
纯度 : 98%
分子量 : 541.18
MDL号 : MFCD31811638
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(46.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.24mL

1.85mL

0.92mL

18.48mL

3.70mL

1.85mL
参考文献

[1]Visnes T, Cázares-Körner A, Hao W, et al. Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation. Science. 2018;362(6416):834-839