Home / Casein Kinase 1 Inhibitors / D 4476

D 4476

Catalog #: 2902
5 Citations Datasheet / COA / SDS
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2902/10
2902/50
D 4476 | CAS No. 301836-43-1 | Casein Kinase 1 Inhibitors
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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)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

The citations listed below are publications that use Tocris products. Selected citations for D 4476 include:

5 Citations: Showing 1 - 5

  1. Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP.
    Authors: Bartley Et al.
    Eneuro  2016;3
  2. GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis.
    Authors: Zhang Et al.
    PLoS Biol  2015;13:e1002129
  3. CK1δ and CK1ε are components of human 40S subunit precursors required for cytoplasmic 40S maturation.
    Authors: Zemp Et al.
    J Cell Sci  2014;127:1242
  4. Pathogen recognition receptor signaling accelerates phosphorylation-dependent degradation of IFNAR1.
    Authors: Qian Et al.
    PLoS Pathog  2011;7:e1002065
  5. Perspectives on Regulatory T Cell Therapies.
    Authors: Probst-Kepper Et al.
    Toxins (Basel)  2009;36:302

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