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TAK-756

Chemical Structure : TAK-756

CAS No.:

TAK-756 (TAK756)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 447.49
Formula C25H25N3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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