Home / Pharmacology / Enzymes / Kinases / Casein Kinase 1 / Casein Kinase 1 Inhibitors / D 4476

D 4476

Cat. No. 2902 5 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 (5)
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for D 4476

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.

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries for D 4476

D 4476 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for D 4476

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for D 4476

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

Preparing Stock Solutions for D 4476

The following data is based on the product molecular weight 398.41. Batch specific molecular weights may vary from batch to batch due to the degree 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

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Product Datasheets for D 4476

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for D 4476

References are publications that support the biological activity of the product.

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.

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View all Casein Kinase 1 Inhibitors

Keywords: D 4476, D 4476 supplier, 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, 2902, Tocris Bioscience

5 Citations for D 4476

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

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

Bartley et al (2016) Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP. Eneuro 3 PMID: 27957526

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

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

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

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

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Literature in this Area

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