Name: AMG 548
Price: 648.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    AMG 548 is a potent and selective inhibitor of p38α with IC50 values of 0.5, 3.6, 2600 and 4100 nM for p38α, p38β, p38γ and p38δ, respectively.
    P38 mitogen-activated protein kinase (p38) is a serine/threonine kinase and is responsive to a variety of cellular stresses including inflammatory cytokines, osmotic shock, ultraviolet light, lipopolysaccharides (LPS) and growth factors. P38α kinase involved in the biosynthesis of TNFα and IL-1β at the transcriptional and translational level [1][2].
    AMG 548 is a potent and selective p38α inhibitor. In the antagonistic enzyme fragment complementation (EFC) and β-catenin-driven luciferase (SuperTOPflash) reporter gene assays, AMG 548 inhibited Wnt/β-catenin signaling, which was due to cross-reactivity with another kinase. AMG 548 inhibited 17 kinases by more than 80%. In U2OS-EFC cells, AMG 548 inhibited CKIδ and CKIε, which played an important role in the activation of Wnt/b-catenin signaling. Also, the concentration of AMG 548 needed to inhibit CKIδ/ε in cells was closely approximate that required to inhibit Wnt/b-catenin signaling in the EFC and TOPflash assays, which suggested AMG 548 inhibited Wnt/b-catenin signaling mediated by the inhibition of CKIδ/ε [3].
    
    [1]. Dominguez C, Powers DA, Tamayo N. p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Devel, 2005, 8(4): 421-430.
    [2]. Lee MR, Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem, 2005, 12(25): 2979-2994.
    [3]. Verkaar F, van der Doelen AA, Smits JF, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol, 2011, 18(4): 485-494.
- Properties
  - Alternative Name
    
    (S)-2-((2-amino-3-phenylpropyl)amino)-3-methyl-5-(naphthalen-2-yl)-6-(pyridin-4-yl)pyrimidin-4(3H)-one
    
    CAS Number
    
    864249-60-5
    
    Molecular Formula
    
    C29H27N5O
    
    Molecular Weight
    
    461.56
    
    Appearance
    
    Yellow solid
    
    Purity
    
    98.00%
    
    Solubility
    
    <49.8mg/ml in DMSO; <49.8mg/ml in ethanol
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

AMG 548

AMG 548

Background

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