Chemical Structure : TAK-756
货号: PC-23560Not For Human Use, Lab Use Only.
TAK-756 is a potent, selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with pIC50 of 8.6, 464/60-fold selective over IRAK1/4.
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TAK-756 is a potent, selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with pIC50 of 8.6, 464/60-fold selective over IRAK1/4.
TAK-756 exhibits a good selectivity score of 0.06 (S(50%)) in a panel of 330 kinases.
TAK-756 inhibits the phosphorylation of NF-κB, a downstream target of TAK1, with IC50 of 0.1 uM in SW982 cells upon activation with IL-1β.
TAK-756 dose-dependently decreases the expression levels of Cxcl1, Mmp3, and Il6 in meniscus, attenuates the inflammatory response triggered by an injection of monosodium urate (MSU) crystals and lipopolysaccharide (LPS) in the joint of naïve rats.
分子量 | 447.49 | |
分子式 | C25H25N3O5 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Langlois JB, et al. J Med Chem. 2024 Nov 22. doi: 10.1021/acs.jmedchem.4c01938.
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