PF 670462

Cat. No. 3316

PF 670462 C19H20FN5.2HCl [950912-80-8]

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Chemical Name: 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine dihydrochloride

Biological Activity

Potent and selective casein kinase 1ε (CK1ε) and CK1δ inhibitor (IC50 values are 7.7 and 14 nM respectively) that displays > 30-fold selectivity over 42 other common kinases. Inhibits PER protein nuclear translocation (EC50 = 290 nM) causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo.

Technical Data

M.Wt:
410.32
Formula:
C19H20FN5.2HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at RT
CAS No:
950912-80-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Bryant et al (2009) A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. Psychopharmacology 203 703. PMID: 19050854.

Sprose et al (2009) Inhibition of casein kinase I ε/δ produces phase shifts in the circadian rhythms of Cynomolgus monkeys. Psychopharmacology 204 735. PMID: 19277609.

Badura et al (2007) An inhibitor of casein kinase Iε induces phase delays in circadian rhythms under free-running and entrained conditions. J.Pharmacol.Exp.Ther. 322 730. PMID: 17502429.

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Citations are publications that use Tocris products. Selected citations for PF 670462 include:

Causton et al (2015) Metabolic cycles in yeast share features conserved among circadian rhythms. Curr.Biol. 25 1056. PMID: 25866393.

Cheong et al (2015) Casein kinase 1α-dependent feedback loop controls autophagy in RAS-driven cancers. J Clin Invest 125 1401. PMID: 25798617.

Kaucka et al (2015) Asymmetry of VANGL2 in migrating lymphocytes as a tool to monitor activity of the mammalian WNT/planar cell polarity pathway. Cell Commun Signal 13 2. PMID: 25627785.

Kurihara et al (2014) Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors. Mol Pain 10 17. PMID: 24612480.

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.

Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832. PMID: 22434859.

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Keywords: PF 670462, supplier, Potent, selective, CK1ε, CK1epsilon, CK1δ, CK1delta, inhibitors, inhibits, Casein, Kinases, 1, PF670462, circadian, rhythms, Tocris Bioscience, Casein Kinase 1 Inhibitor products

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