218719
Casein Kinase I Inhibitor III, PF-4800567
The Casein Kinase I Inhibitor III, PF-4800567 controls the biological activity of Casein Kinase I. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Casein Kinase I Inhibitor III, PF-4800567, 3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
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关于此项目
经验公式（希尔记法）:
C17H18ClN5O2
化学文摘社编号:
分子量:
359.81
UNSPSC Code:
12352200
NACRES:
NA.54
MDL number:
InChI
1S/C17H18ClN5O2/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21)
InChI key
AUMDBEHGJRZSOO-UHFFFAOYSA-N
SMILES string
NC1=NC=NC2=C1C(COC3=CC=CC(Cl)=C3)=NN2C4CCOCC4
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
beige
solubility
DMSO: 50 mg/mL
shipped in
wet ice
Quality Level
General description
A cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC50 = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Meng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA24, 15240.
Etchegaray, J.P., et al. 2010. PLoS One5, e10303.
Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther.330, 430.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther.322, 730.
Etchegaray, J.P., et al. 2010. PLoS One5, e10303.
Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther.330, 430.
Badura, L., et al. 2007. J. Pharmacol. Exp. Ther.322, 730.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
wgk
WGK 2
flash_point_f
Not applicable
存储类别
11 - Combustible Solids
flash_point_c
Not applicable
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