Name: TAK-715
Price: 268.00 USD

- Overview
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    Background
    
    TAK-715 is a selective inhibitor of p38 MAPK with IC50 value of 7.1 nM [1].
    p38 mitogen-activated protein (MAP) kinases (p38 MAPKs) are a class of mitogen-activated protein kinases and play an important role in controlling cellular responses to cytokines and stress. Four p38 MAPKs contain members, p38-α (MAPK14), p38-β (MAPK11), p38-γ (MAPK12/ERK6), and p38-δ (MAPK13/SAPK4), have been identified. Abnormal expression of p38 MAPKs are correlated with a variety of chronic inflammatory diseases and their inhibitors are regarded as promising targets in clinical [1] [2].
    TAK-715 is a potent p38 MAPK inhibitor and has a different selectivity with the reported p38 MAPK inhibitor VX-745. When tested with human monocytic THP-1 cells, administration of TAK-715 exhibited inhibition on p38MAPKα with IC50 value of 7.1 nM [1]. In HEK293T, U2OS, and F9 cells, TAK-715 was used to inhibit p38 MAPK activity and concluded that p38 MAPK had no function in Wnt/β-catenin signaling pathway [2].
    In adjuvant-induced rheumatoid arthritis rat model, administration of TAK-715 at dose of 10 mg/kg significantly decreased LPS-induced stimulated release of TNF-α (87.6%) by inhibiting p38 MAPK activity [1].
    
    [1]. Miwatashi, S., et al., Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem, 2005. 48(19): p. 5966-79.
    [2]. Verkaar, F., et al., Inhibition of Wnt/beta-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Idelta/varepsilon. Chem Biol, 2011. 18(4): p. 485-94.
- Properties
  - Alternative Name
    
    N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]pyridin-2-yl]benzamide
    
    CAS Number
    
    303162-79-0
    
    Molecular Formula
    
    C24H21N3OS
    
    Molecular Weight
    
    399.52
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥40 mg/mL in DMSO; insoluble in H2O; ≥12.13 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

TAK-715

TAK-715

Background

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