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首页-小分子抑制剂&激动剂-NF-κB Pathway-TAK1-TAK-756
TAK-756

Chemical Structure : TAK-756

CAS No.:

TAK-756 (TAK756)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 447.49
分子式 C25H25N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(5-(6-((Cis-4-Hydroxycyclohexyl)oxy)-2-Methyl-1-Oxoisoindolin-5-yl)isoxazol-3-yl)benzamide

参考文献

1. Langlois JB, et al. J Med Chem. 2024 Nov 22. doi: 10.1021/acs.jmedchem.4c01938.

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