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D 4476

Cayman Chemical Item Number 13305

Casein Kinase I Inhibitor (CAS 301836-43-1)

D 4476 (CAS 301836-43-1)

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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

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 Rep 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 408 297-315 (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 2811-2821 (2008).

4 MacLaine, N.J., Øster, 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. J Biol Chem 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 b1 (TGF-b1) type 1 receptor (ALK5). J Med Chem 45(5) 999-1001 (2002).

Synonyms
  • Casein Kinase I Inhibitor
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
Molecular Formula C23H18N4O3
Formula Weight 398.4
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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NC(=O)​c1ccc(cc1)​c1nc(c2ccc3OCCOc3c2)​c([nH]​1)​c1ccccn1

Background Reading

MacLaine, N.J., Øster, 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. J Biol Chem 283(42) 28563-28573 (2008).

Callahan, J.F., Burgess, J.L., Fornwald, J.A., et al. Identification of novel inhibitors of the transforming growth factor b1 (TGF-b1) type 1 receptor (ALK5). J Med Chem 45(5) 999-1001 (2002).

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 Rep 5(1) 60-65 (2004).

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

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 2811-2821 (2008).

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D 4476 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $19.00 $0.00
5 mg $86.00 $0.00
10 mg $152.00 $0.00
50 mg $665.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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