Name: D4476
Price: 258.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    D4476 is a relatively specific and cell-permeant inhibitor of CK1 and ALK5 with respective IC50 values of 0.3 and 0.5 μM at 0.1 mM ATP in vitro.[1]
    CK1 (casein kinase 1) phosphorylates serine residues that are located close to another phosphoserine in multisite phosphorylation domains (MPDs). D4476 may be an ATP-competitive inhibitor of CK1. It weakly inhibits SAPK2a/p38 and does not inhibit PKB or SGK. In H4IIE cells, the site-specific phosphorylation (Ser322 and Ser325) of FOXO1a was inhibited at 50 and 125 μM, which reduced the initial rate of nuclear exclusion[1]. In Hela cells, the phosphorylation(Ser185) of RhoB caused by CK1 was inhibited by D4476 at 50 μM then the RhoB-dependent actin fiber formation was subsequently activated[2]. D4476 treatment has been observed to result in a partial p53-dependent growth arrest in HCT116 cells.[3]
    
    1. G. Rena, J. Bain, M. Elliott and P. Cohen, EMBO Rep 2004, 5, 60-65.
    2. V. Tillement, I. Lajoie-Mazenc, A. Casanova, C. Froment, M. Penary, D. Tovar, R. Marquez, B. Monsarrat, G. Favre and A. Pradines, Exp Cell Res 2008, 314, 2811-2821.
    3. A. S. Huart, N. J. MacLaine, D. W. Meek and T. R. Hupp, J Biol Chem 2009, 284, 32384-32394.
- Properties
  - Alternative Name
    
    Casein Kinase I Inhibitor;D 4476;D-4476; 4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide
    
    CAS Number
    
    301836-43-1
    
    Molecular Formula
    
    C23H18N4O3
    
    Molecular Weight
    
    398.41
    
    Appearance
    
    A solid
    
    Purity
    
    99.70%
    
    Solubility
    
    insoluble in H2O; ≥19.9 mg/mL in DMSO; ≥41.5 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mansour TA, Lucot K, et al. "Whole genome variant association across 100 dogs identifies a frame shift mutation in DISHEVELLED 2 which contributes to Robinow-like syndrome in Bulldogs and related screw tail dog breeds." PLoS Genet. 2018 Dec 6;14(12):e1007850. PMID:30521570

D4476

D4476

Background

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