D 4476

Pricing Availability Delivery Time Qty
Cat.No. 2902 - D 4476 | C23H18N4O3 | CAS No. 301836-43-1
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% (HPLC)
Datasheet
Citations (4)
Literature

Biological Activity

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.

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries

D 4476 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 398.41
Formula C23H18N4O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 301836-43-1
PubChem ID 6419753
InChI Key DPDZHVCKYBCJHW-UHFFFAOYSA-N
Smiles O=C(N)C4=CC=C(C=C4)C1=NC(C2=CC(OCCO5)=C5C=C2)=C(C3=NC=CC=C3)N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.84 100
ethanol 19.92 50

Preparing Stock Solutions

The following data is based on the product molecular weight 398.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.51 mL 12.55 mL 25.1 mL
5 mM 0.5 mL 2.51 mL 5.02 mL
10 mM 0.25 mL 1.25 mL 2.51 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

Callahan et al (2002) Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5). J.Med.Chem. 45 999 PMID: 11855979

Rena et al (2004) D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 5 60 PMID: 14710188

Bain et al (2007) The selectivity of protein kinase inhibitors: a further update. Biochem.J. 408 297 PMID: 17850214


If you know of a relevant reference for D 4476, please let us know.

View Related Products by Product Action

View all Casein Kinase 1 Inhibitors

Keywords: Selective CK1 inhibits inhibitors TGF-βRI TGF-β TGF-betaRI TGFbRI TGFbR1 tgf-b1Casein Kinase 1 Kinases Transforming Growth Factors Beta Receptors TGF-beta RSTK Receptor Serine/Threonine RSTKs D4476 GlaxoSmithKline GSK Casein Kinase 1

4 Citations for D 4476

Citations are publications that use Tocris products. Selected citations for D 4476 include:

Qian et al (2011) Pathogen recognition receptor signaling accelerates phosphorylation-dependent degradation of IFNAR1. PLoS Pathog 7 e1002065 PMID: 21695243

Probst-Kepper et al (2009) Perspectives on Regulatory T Cell Therapies. Toxins (Basel) 36 302 PMID: 21076548

Zhang et al (2015) GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis. PLoS Biol 13 e1002129 PMID: 25860027

Zemp et al (2014) CK1δ and CK1ε are components of human 40S subunit precursors required for cytoplasmic 40S maturation. J Cell Sci 127 1242 PMID: 24424021


Do you know of a great paper that uses D 4476 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease

Pathways for D 4476

Protocols

TODO: Add Protocols