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Takinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Takinib图片
CAS NO:1111556-37-6
规格:98%
分子量:322.36
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Takinib是一种有效且有选择性的TAK1抑制剂,其IC50值为9.5nM。
CAS:1111556-37-6
分子式:C18H18N4O2
分子量:322.36
纯度:98%
存储:Store at -20°C

Background:

Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM.


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 significantly but does not influence total protein levels. Takinib inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun in a dose-dependent manner. Takinib shows an almost complete inhibition of IL-6 secretion at micromolar concentrations following 24 hr of treatment in the presence of TNF-α[1].



[1]. Totzke J, et al. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17;24(8):1029-1039.