218705
Casein Kinase I Inhibitor, D4476
InSolution, ≥95%
Synonym(s):
InSolution Casein Kinase I Inhibitor, D4476
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About This Item
Empirical Formula (Hill Notation):
C23H18N4O3
Molecular Weight:
398.41
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
shipped in
wet ice
storage temp.
−20°C
General description
A cell-permeable, potent, and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 200 nM from S. pombe; 0.3 µM for CK1δ) and ALK5 (IC50 = 500 nM). A weak inhibitor of p38α MAP kinase (IC50 = 12 µM) and several other kinases tested, including PKB, SGK, and GSK-3β. Suppresses the site-specific phosphorylation (Ser322 and Ser325) and nuclear exclusion of FOXO1A in H4IIE hepatoma cells. Shown to be ~10-fold more potent than IC261 (Cat. No. 400090; IC50 = 2.5 µM for CK1).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CK1, CK1d
CK1, CK1d
Product competes with ATP.
Reversible: no
Target IC50: 0.2 µM, 0.3 µM against CK1, CK1d, respectively
Packaging
Packaged under inert gas
Please refer to vial label for lot-specific concentration.
Warning
Toxicity: Irritant (B)
Physical form
A 10 mM (1 mg/251 µl) solution of Casein Kinase I Inhibitor, D4476 (Cat. No. 218696) in DMSO
Reconstitution
Following initial use, aliquot and refrigerate (4°C).
Other Notes
Rena, G., et al. 2004. EMBO Reports5, 60.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Certificates of Analysis (COA)
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Ali Vural et al.
Journal of cell science, 133(17) (2020-08-02)
Activator of G-protein signaling 3 (AGS3, encoded by GPSM1) was discovered as a one of several receptor-independent activators of G-protein signaling, which are postulated to provide a platform for divergence between canonical and noncanonical G-protein signaling pathways. Similarly, Dishevelled (DVL)
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