Chemical Name: 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine dihydrochloride
Biological ActivityPF 670462 is a 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
An inhibitor of casein kinase Iε induces phase delays in circadian rhythms under free-running and entrained conditions.
Badura et al.
Inhibition of casein kinase I ε/δ produces phase shifts in the circadian rhythms of Cynomolgus monkeys.
Sprose et al.
A role for casein kinase 1 epsilon in the locomotor stimulant response to metha.
Bryant et al.
Citations for PF 670462
The citations listed below are publications that use Tocris products. Selected citations for PF 670462 include:
11 Citations: Showing 1 - 10
Oncogenic RAS-induced CK1α drives nuclear FOXO proteolysis.
Authors: Zhang Et al.
Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of dFdCyd-Resistant Pancreatic Cancer Cell Growth.
Authors: Krulikas Et al.
SLAS Discov 2018;23:850
Lack of Casein Kinase 1 Delta Promotes Genomic Instability - The Accumulation of DNA Damage and Down-Regulation of Checkpoint Kinase 1.
Authors: Greer Et al.
PLoS One 2017;12:e0170903
Metabolic cycles in yeast share features conserved among circadian rhythms.
Authors: Causton Et al.
Asymmetry of VANGL2 in migrating lymphocytes as a tool to monitor activity of the mammalian WNT/planar cell polarity pathway.
Authors: Kaucka Et al.
Cell Commun Signal 2015;13:2
Casein kinase 1α-dependent feedback loop controls autophagy in RAS-driven cancers.
Authors: Cheong Et al.
J Clin Invest 2015;125:1401
CK1δ and CK1ε are components of human 40S subunit precursors required for cytoplasmic 40S maturation.
Authors: Zemp Et al.
J Cell Sci 2014;127:1242
Alleviation of behavioral hypersensitivity in mouse models of inflammatory pain with two structurally different casein kinase 1 (CK1) inhibitors.
Authors: Kurihara Et al.
Mol Pain 2014;10:17
Circadian and circalunar clock interactions in a marine annelid.
Authors: Zantke Et al.
PLoS One 2013;5:99
Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra.
Authors: Zhang Et al.
Curr Biol 2013;23:1863
Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.
Authors: Schepetkin Et al.
Mol Pharmacol 2012;81:832
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