Inhibitor of CK1 and ALK5
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D 4476

Item No. 13305

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)1H-imidazol-2-yl]-benzamide
CAS Number
301836-43-1
Synonyms
  • Casein Kinase I Inhibitor
Molecular Formula
C23H18N4O3
Formula Weight
398.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/mlEthanol: 10 mg/ml
λmax
329 nm
SMILES
NC(=O)c1ccc(cc1)c1nc(c2ccc3OCCOc3c2)c([nH]1)c1ccccn1
InChi Code
InChI=1S/C23H18N4O3/c24-22(28)14-4-6-15(7-5-14)23-26-20(21(27-23)17-3-1-2-10-25-17)16-8-9-18-19(13-16)30-12-11-29-18/h1-10,13H,11-12H2,(H2,24,28)(H,26,27)
InChi Key
DPDZHVCKYBCJHW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    D 4476 is a cell-permeant inhibitor of casein kinase 1 (CK1; IC50 = 200 nM from S. pombe,1 300 nM for CK1δ2). It is a less effective inhibitor of PKD1 (IC50 = 9.1 μM) and p38α MAPK (IC50 = 5.8 μM), and only weakly affects the activities of a panel of kinases tested.2 D 4476 blocks CK1-mediated phosphorylation of FOXO1a,1 RhoB,3 and p53.4 As an inhibitor of ALK5, D 4476 prevents Smad3 activation and suppresses TGF-β1-induced gene expression without cytotoxicity in A498 cells.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rena, G., Bain, J., Elliot, M., et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO reports 5(1), 60-65 (2004).

    2. Bain, J., Plater, L., Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochem. J. 408(3), 297-315 (2007).

    3. Tillement, V., Lajoie-Mazenc, I., Casanova, A., et al. Phosphorylation of RhoB by CK1 impedes actin stress fiber organization and epidermal growth factor receptor stabilization. Exp. Cell Res. 314(15), 2811-2821 (2008).

    4. MacLaine, N.J., Oster, B., Bundgaard, B., et al. A central role for CK1 in catalyzing phosphorylation of the p53 transactivation domain at serine 20 after HHV-6B viral infection. The Journal of Biological Chemisty 283(42), 28563-28573 (2008).

    5. Callahan, J.F., Burgess, J.L., Fornwald, J.A., et al. Identification of novel inhibitors of the transforming growth factor ß1 (TGF-ß1) type 1 receptor (ALK5). J. Med. Chem. 45(5), 999-1001 (2002).