D 4476

Catalog # Availability Size / Price Qty
2902/10
2902/50
D 4476 | CAS No. 301836-43-1 | Casein Kinase 1 Inhibitors
1 Image
Description: Selective CK1 inhibitor. Also inhibits TGF-βRI

Chemical Name: 4-[4-(2,3-Dihydro-1,4-benzodioxin-6-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide

Purity: ≥99%

Product Details
Citations (5)
Supplemental Products
Reviews

Biological Activity

D 4476 is a selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) that displays > 20-fold selectivity over SAPK2/p38 and a much greater selectivity over all other protein kinases tested. Suppresses site-specific phosphorylation and nuclear exclusion of FOXO1a.

Technical Data

M.Wt:
398.41
Formula:
C23H18N4O3
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
301836-43-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of GlaxoSmithKline

Background References

  1. Csnk1a1 inhibition has p53-dependent therapeutic efficacy in acute myeloid leukemia.
    Jaras M, Miller P, Chu L, Puram R, Fink E, Schneider R, Al-Shahrour F, Pena P, Breyfogle L, Hartwell K, McConkey M, Cowley G, Root D, Kharas M, Mullally A, Ebert B
    J Exp Med, 2014;211(4):605-12.
  2. The selectivity of protein kinase inhibitors: a further update.
    Bain et al.
    Biochem.J., 2007;408:297
  3. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a.
    Rena et al.
    EMBO Rep., 2004;5:60
  4. Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5).
    Callahan et al.
    J.Med.Chem., 2002;45:999

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Citations for D 4476

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