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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.
Sold with the permission of GlaxoSmithKline
Compound Libraries for D 4476
Technical Data for D 4476
|Storage||Store at +4°C|
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|
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.
|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|
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
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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:
Bartley et al (2016) Mammalian FMRP S499 Is Phosphorylated by CK2 and Promotes Secondary Phosphorylation of FMRP. Eneuro 3 PMID: 27957526
Zhang et al (2015) GSK3β-Dzip1-Rab8 cascade regulates ciliogenesis after mitosis. PLoS Biol 13 e1002129 PMID: 25860027
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
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? Please let us know.
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Literature in this Area
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