PF 670462
Chemical Name: 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine dihydrochloride
Purity: ≥99%
Biological Activity
PF 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Tiam1 regulates the Wnt/Dvl/Rac1 signaling pathway and the differentiation of midbrain dopaminergic neurons.
Cajanek L, Ganji R, Henriques-Oliveira C, Theofilopoulos S, Konik P, Bryja V, Arenas E
Mol Cell Biol, 2013;33(1):59-70. -
Asymmetry of VANGL2 in migrating lymphocytes as a tool to monitor activity of the mammalian WNT/planar cell polarity pathway.
Kaucka M, Petersen J, Janovska P, Radaszkiewicz T, Smyckova L, Daulat A, Borg J, Schulte G, Bryja V
Cell Commun Signal, 2015;13(0):2. -
Combined Pharmacological and Genetic Manipulations Unlock Unprecedented Temporal Elasticity and Reveal Phase-Specific Modulation of the Molecular Circadian Clock of the Mouse Suprachiasmatic Nucleus
J Neurosci, 2016;36(36):9326-41. -
An inhibitor of casein kinase Iε induces phase delays in circadian rhythms under free-running and entrained conditions.
Badura et al.
J.Pharmacol.Exp.Ther., 2007;322:730 -
Inhibition of casein kinase I ε/δ produces phase shifts in the circadian rhythms of Cynomolgus monkeys.
Sprose et al.
Psychopharmacology, 2009;204:735 -
A role for casein kinase 1 epsilon in the locomotor stimulant response to metha.
Bryant et al.
Psychopharmacology, 2009;203:703
Product Datasheets
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Citations for PF 670462
The citations listed below are publications that use Tocris products. Selected citations for PF 670462 include:
12 Citations: Showing 1 - 10
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The Wnt pathway protein Dvl1 targets Somatostatin receptor 2 for lysosome-dependent degradation.
Authors: Carr Et al.
J.Biol.Chem. 2023;
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Oncogenic RAS-induced CK1α drives nuclear FOXO proteolysis.
Authors: Zhang Et al.
Oncogene 2018;37:363
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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
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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
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Metabolic cycles in yeast share features conserved among circadian rhythms.
Authors: Causton Et al.
Curr.Biol. 2015;25:1056
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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
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Casein kinase 1α-dependent feedback loop controls autophagy in RAS-driven cancers.
Authors: Cheong Et al.
J Clin Invest 2015;125:1401
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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
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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
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Circadian and circalunar clock interactions in a marine annelid.
Authors: Zantke Et al.
PLoS One 2013;5:99
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Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra.
Authors: Zhang Et al.
Curr Biol 2013;23:1863
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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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