Molecular structure of Casein Kinase I Inhibitor, D4476, CAS Number: 301836-43-1
Casein Kinase I Inhibitor, D4476 (CAS 301836-43-1)
See product citations (6)
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.
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SDS & Certificate of Analysis
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 TGFbeta RI (TGF-betatype-I receptor, ALK5). Weak inhibitor of Polycystin-1 (PKD1), p38α (p38alpha 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 TGFbeta RI, D4476 prevents Smad3 activation and suppresses TGFbeta RI gene expression without cytotoxicity in A498 cells. In HeLa cells, Casein Kinase I Inhibitor, D4476 has been used to inhibit CK-1 phosphorylation of RhoB but not RhoA or RhoC activating RhoB dependent actin fiber formation. Casein Kinase I Inhibitor, D4476 has been observed to block the Wnt-3a-induced phosphorylation and shift in electrophoretic migration of Dvl-1(dishevelled, Dvl).
Casein Kinase I Inhibitor, D4476 (CAS 301836-43-1) References
- Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). | Callahan, JF., et al. 2002. J Med Chem. 45: 999-1001. PMID: 11855979
- D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. | Rena, G., et al. 2004. EMBO Rep. 5: 60-5. PMID: 14710188
- Wnt-3a utilizes a novel low dose and rapid pathway that does not require casein kinase 1-mediated phosphorylation of Dvl to activate beta-catenin. | Bryja, V., et al. 2007. Cell Signal. 19: 610-6. PMID: 17027228
- The selectivity of protein kinase inhibitors: a further update. | Bain, J., et al. 2007. Biochem J. 408: 297-315. PMID: 17850214
- Phosphorylation of RhoB by CK1 impedes actin stress fiber organization and epidermal growth factor receptor stabilization. | Tillement, V., et al. 2008. Exp Cell Res. 314: 2811-21. PMID: 18590726
- A central role for CK1 in catalyzing phosphorylation of the p53 transactivation domain at serine 20 after HHV-6B viral infection. | MacLaine, NJ., et al. 2008. J Biol Chem. 283: 28563-73. PMID: 18669630
- CK1 inhibitor affects in vitro maturation and developmental competence of bovine oocytes. | Shi, P., et al. 2019. Reprod Domest Anim. 54: 1104-1112. PMID: 31155763
- Stimulation of calcium influx and CK1α by NF-κB antagonist [6]-Gingerol reprograms red blood cell longevity. | Alamri, HS., et al. 2021. J Food Biochem. 45: e13545. PMID: 33145778
- Lenalidomide downregulates ACE2 protein abundance to alleviate infection by SARS-CoV-2 spike protein conditioned pseudoviruses. | Su, S., et al. 2021. Signal Transduct Target Ther. 6: 182. PMID: 33972500
- Csnk1a1 inhibition modulates the inflammatory secretome and enhances response to radiotherapy in glioma. | Liu, G., et al. 2021. J Cell Mol Med. 25: 7395-7406. PMID: 34216174
- Casein Kinase-1-Alpha Inhibitor (D4476) Sensitizes Microsatellite Instable Colorectal Cancer Cells to 5-Fluorouracil via Authophagy Flux Inhibition. | Siri, M., et al. 2021. Arch Immunol Ther Exp (Warsz). 69: 26. PMID: 34536148
- Casein kinase I inhibitor D4476 influences autophagy and apoptosis in chloroquine-induced adult retinal pigment epithelial-19 cells. | Nguyen Hoang, AT., et al. 2022. Exp Eye Res. 218: 109004. PMID: 35219693
- Knockdown of Csnk1a1 results in preimplantation developmental arrest in mice. | Ma, Z., et al. 2023. Theriogenology. 198: 30-35. PMID: 36542875
Inhibitor of:
APBB1IP, Casein Kinase, casein kinase I epsilon, casein kinase Iα, casein kinase Iγ1, casein kinase Iγ2, CASPR2, Cdc10, CELSR1, CLK2, CSNK1A1L, DCC, Ethanolamine kinase 2, Freud-1, IGSF4B, KRTAP10-4, LRRC10B, NEGR1, Olr22, p38 alpha, PCDH11X, Pilr-β2, Polycystin-1, POU3F, PTPN21, Rab 35, Ser/Thr Protein Kinase, SLITRK4, Tdpoz4, TGF beta RI, and WDPCP.Activator of:
α T-catenin, AAK1, ANKRD40, CAB39L, casein kinase Iγ3, CCDC64B, CCDC78, Clik1, CLK3, FRA10AC1, frizzled-5, glypican-4, MFSD7, Msi2, Nek11, nm23-H5, NOB1P, plexin-B2, RBM42, Ribosomal Protein L14, SBF2, SGK, Smad2, UBL4A, and ZNF585A.Substrate of:
LTC4 synthase.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Casein Kinase I Inhibitor, D4476, 1 mg | sc-202522 | 1 mg | $99.00 |