Casein Kinase I Inhibitor, D4476 CAS: 301836-43-1
MF: C23H18N4O3
MW: 398.41

Casein Kinase I Inhibitor, D4476 (CAS 301836-43-1)

Casein Kinase I Inhibitor, D4476 | CAS 301836-43-1 is rated 5.0 out of 5 by 1.
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Alternate Names: 4-[4-(2,3-dihydro-1, 4-benzodioxin-6-yl)-5-(2-pyridinyl)1H-imidazol-2-yl]-benzamide
Application: Casein Kinase I Inhibitor, D4476 is a cell-permeable triaryl substituted imidazolo compound that acts as a selective inhibitor of casein kinase 1 (CK1)
CAS Number: 301836-43-1
Purity: ≥98%
Molecular Weight: 398.41
Molecular Formula: C23H18N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Casein Kinase I Inhibitor, D4476 is a cell-permeable triaryl substituted imidazolo compound that acts as a selective inhibitor of casein kinase 1 (CK1) and TGFβ RI (TGF-βtype-I receptor, ALK5). Weak inhibitor of Polycystin-1 (PKD1), p38α (p38α MAPK) and only weakly affects the activities of kinases, including Akt1 (PKB), SGK and GSK-3b. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FKHR (FOXO1a) in H4IIE hepatoma cells. As an inhibitor of TGFβ RI, D4476 prevents Smad3 activation and suppresses TGFβ RI gene expression without cytotoxicity in A498 cells. In HeLa cells D4476 has been used to inhibit CK-1 phosphorylation of RhoB but not RhoA or RhoC activating RhoB dependent actin fiber formation. D4476 has been observed to block the Wnt-3a-induced phosphorylation and shift in electrophoretic migration of Dvl-1(dishevelled, Dvl).


References

1. Callahan, J.F., et al. 2002. J. Med. Chem. 45: 999-1001. PMID: 11855979
2. Rena, G., et al. 2004. EMBO Rep. 5: 60-65. PMID: 14710188
3. Bain, J., et al. 2007. Biochem. J. 408: 297-315. PMID: 17850214
4. Tillement, V., et al. 2008. Exp. Cell Res. 314: 2811-2821. PMID: 18590726
5. MacLaine, N.J., et al. 2008. J. Biol. Chem. 283: 28563-28573. PMID: 18669630
6. Bryja, V., et al. 2007. Cell. Signal. 19: 610-616. PMID: 17027228

Physical State :
Solid
Solubility :
Soluble in DMSO (~20 mg/ml), ethanol (50 mM), and 1:10 DMSO:PBS (pH 7.2) (0.1 mg/ml). Insoluble in water.
Storage :
Store at 4° C
Melting Point :
321.63° C (Predicted)
Boiling Point :
~675.0° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
CK1: IC50 = 0.2 µM; CK1δ: IC50 = 0.3 µM; ALK5: IC50 = 0.5 µM; p38α MAP kinase: IC50 = 12 µM; PKD1: IC50 = 9.1 µM
pK Values :
pKa: 10.05, pKb: 3.30
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
MDL Number :
MFCD09037526
SMILES :
C1COC2=C(O1)C=CC(=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

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Certificate of Analysis

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Casein Kinase I Inhibitor, D4476 (CAS 301836-43-1)  Product Citations

See how others have used Casein Kinase I Inhibitor, D4476 (CAS 301836-43-1). Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 30142917  Hernandez-Valencia, J. et al. 2018. Nutrients. 10:

PMID: # 23606524  León-Espinosa, G. et al. 2013. Journal of neuroscience research. 91: 954-62.

PMID: # 14710188  Rena, G. et al. 2004. EMBO Rep. 5: 60-65.

PMID: # 11855979  Callahan, JF. et al. 2002. J. Med. Chem. 45: 999-1001.

PMID: # 29202451  JCI Insight.

PMID: # 32460168  EBioMedicine. 56: 102795.

Citations 1 to 6 of 6 total
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Rated 5 out of 5 by from Rena Rena, G. et al. (PubMed 14710188) found that Casein Kinase I Inhibitor (D4476) specifically inhibited the phosphorylation of endogenous forkhead box transcription factor O1a (FOXO1a) on Ser322 and Ser325 within its multisite phosphorylation domains, without affecting the phosphorylation of other sites. -SCBT Publication Review
Date published: 2015-01-16
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