D 4476

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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 (5)
Reviews
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.

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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View Related Products by Product Action

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:

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

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

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


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