Takinib
| CAS号 | 1111556-37-6 | 货号 | BCP20873 |
| 中文名 | Takinib | ||
| 英文名 | Takinib | ||
| 中文别名 | |||
| 英文别名 | EDHS-206; EDHS 206; EDHS206; | ||
| 分子式 | C18H18N4O2 | 分子量 | 322.36 |
| 生物活性 | Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM. IC50 & Target: IC50: 9.5 nM (TAK1)[1] In Vitro: At 10 mM, Takinib shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. Analysis reveals that increasing concentrations of Takinib leads to a decrease in Vmax while maintaining KM. When the enzyme is activated with 5 mM ATP for 3 hr, the same Vmax is reached for 0, 10, 50, and 100 nM Takinib, and KM increases for these concentrations, which implies that Takinib is an ATP-competitive inhibitor if TAK1 is ATP activated. Importantly, results show that Takinib inhibits the function of both activated and un-activated TAK1 with identical potency. TNF-α stimulation in the presence of Takinib induces caspase activity in MDA-MB-231 cells in a dose-dependent manner, whereas unstimulated cells do not upregulate caspase activity. Takinib reduces phosphorylation significantl | ||
| 信号通路 | MAPK Pathway NFκB | ||
| 靶 点 | MAP3K TAK1 | ||
结构式
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