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.
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- Formule: C25H25N3O5
- Masse moléculaire:447.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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TAK1 8.6 (pIC50) |
NF-κB |
MMP-3 |
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 S50% 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.
| Species | Dose | Route | T1/2 (Elimination) |
|---|---|---|---|
| Rat[1] | 250 μg | o.a. | 93 ± 3 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis/OrlRj (female, 8-10 weeks of age, joint inflammation model)[1]
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Dosage:15-240 μg per knee joint
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Administration:intra-articular injection; single dose
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Result:Reduced CXCL1 levels in synovial fluid by > 90% at the 15 μg dose, with full response at doses ≥ 60 μg.
Produced dose-dependent reductions in CXCL1 and IL6 gene expression in meniscal tissue.
Reduced MMP3 gene expression in meniscal tissue at doses ≥ 30 μg (statistically significant).
Chemical Information
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Masse moléculaire 447.48
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Formule C25H25N3O5
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SMILES
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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TAK-756 Related Classifications
HY-169949 Related Classifications
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- TAK-756
- TAK756
- TAK 756
- MAP3K
- NF-κB
- MMP
- Leukotriene Receptor
- interleukin-1 receptor-associated kinases 4
- TAK1
- inflammatory joint disease
- IRAK4
- HEK293 cells
- IRAK1
- SW982 human synoviosarcoma cells
- interleukin-1 receptor-associated kinases 1
- transforming growth factor β-activated kinase 1
- C20A4 human chondrocytes
- Inhibitor
- inhibitor
- inhibit