TAK-756 

TAK-756 is a selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with a target pIC₅₀ of 8.6. TAK-756 can inhibit TAK1 autophosphorylation and downstream NF-κB phosphorylation, suppress the production of inflammatory and catabolic factors such as MMP-3 and IL-6. TAK-756 exhibits anti-inflammatory effects in a rat joint inflammation model. TAK-756 can be used for the research of inflammatory joint disease, osteoarthritis^[1].

TAK-756 potently inhibits the purified TAK1 enzyme in a biochemical assay with a pIC₅₀ of 8.6, and is highly selective for TAK1 over the purified IRAK1 (464-fold) and IRAK4 enzymes in biochemical assays.^[1].
TAK-756 (20 h) inhibits TAK1 autophosphorylation in HEK293 cells overexpressing TAK1 with a pAC₅₀ of 7.8^[1].
TAK-756 inhibits MMP3 production in C20A4 human chondrocytes with a pAC₅₀ of 7.1^[1].
TAK-756 inhibits IL6 production in SW982 human synoviosarcoma cells with a pAC₅₀ of 7.1^[1].
TAK-756 (1 μM) exhibits good kinome-wide selectivity, with a selectivity score S_50% of 0.06 when tested against 330 kinases, showing strong inhibition of only 5 kinases^[1].
TAK-756 (0.01-10 μM; 1 h pre-incubation) dose-dependently inhibits IL-1β-induced NF-κB phosphorylation in SW982 human synoviosarcoma cells with an IC₅₀ of ~0.1 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAK-756 (15-240 μg per knee joint; intra-articular injection; single dose) delivered via single intra-articular injection (15-240 μg per knee) 72 h prior to inflammation induction in female Lewis/OrlRj rats produces dose-dependent anti-inflammatory and anticatabolic effects, including reduced CXCL1 levels, and reduced CXCL1, IL6 and MMP3 gene expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

447.48

C₂₅H₂₅N₃O₅

O=C(C1=CC(C2=NOC(C3=CC(CN4C)=C(C=C3O[C@@H]5CC[C@@H](CC5)O)C4=O)=C2)=CC=C1)N

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• [1]. Langlois JB, et al. Identification of TAK-756, A Potent TAK1 Inhibitor for the Treatment of Osteoarthritis through Intra-Articular Administration. J Med Chem. 2024;67(23):21163-21185.  [Content Brief]