TH5487 is selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with IC50 of 342 nM.
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产品名称 | Ferroptosis ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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Ferrostatin-1 |
++
Ferroptosis, EC50: 60 nM |
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Liproxstatin-1 |
+++
ferroptosis, IC50: 22 nM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 2304947-71-3 |
分子式 | C19H18BrIN4O2 |
分子量 | 541.18 |
别名 | |
运输 | 蓝冰 |
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 |