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Submit ReviewPF 670462
Description: Potent and selective CK1ε and CK1δ inhibitor
Chemical Name: 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for PF 670462
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.
Compound Libraries for PF 670462
PF 670462 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 670462
| M. Wt | 410.32 |
| Formula | C19H20FN5.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 950912-80-8 |
| PubChem ID | 51049607 |
| InChI Key | PSNKGVAXBSAHCH-UHFFFAOYSA-N |
| Smiles | NC1=NC=CC(C2=C(C4=CC=C(F)C=C4)N=CN2C3CCCCC3)=N1.Cl.Cl |
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.
Solubility Data for PF 670462
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.03 | 100 |
Preparing Stock Solutions for PF 670462
The following data is based on the product molecular weight 410.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.44 mL | 12.19 mL | 24.37 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.87 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets for PF 670462
References for PF 670462
References are publications that support the biological activity of the product.
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
Bryant et al (2009) A role for casein kinase 1 epsilon in the locomotor stimulant response to metha. 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
If you know of a relevant reference for PF 670462, please let us know.
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Keywords: PF 670462, PF 670462 supplier, Potent, selective, CK1ε, CK1epsilon, CK1δ, CK1delta, inhibitors, inhibits, Casein, Kinases, 1, PF670462, circadian, rhythms, Kinase, 3316, Tocris Bioscience
12 Citations for PF 670462
Citations are publications that use Tocris products. Selected citations for PF 670462 include:
Greer et al (2017) Lack of Casein Kinase 1 Delta Promotes Genomic Instability - The Accumulation of DNA Damage and Down-Regulation of Checkpoint Kinase 1. PLoS One 12 e0170903 PMID: 28125685
Causton et al (2015) Metabolic cycles in yeast share features conserved among circadian rhythms. Curr.Biol. 25 1056 PMID: 25866393
Zhang et al (2013) Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra. Curr Biol 23 1863 PMID: 24076244
Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832 PMID: 22434859
Zhang et al (2018) Oncogenic RAS-induced CK1α drives nuclear FOXO proteolysis. Oncogene 37 363 PMID: 28945225
Krulikas et al (2018) Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of dFdCyd-Resistant Pancreatic Cancer Cell Growth. SLAS Discov 23 850 PMID: 29742358
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
Carr et al (2023) The Wnt pathway protein Dvl1 targets Somatostatin receptor 2 for lysosome-dependent degradation. J.Biol.Chem. PMID: 36965619
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
Zantke et al (2013) Circadian and circalunar clock interactions in a marine annelid. PLoS One 5 99 PMID: 24075994
Do you know of a great paper that uses PF 670462 from Tocris? Please let us know.
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Cell Cycle and DNA Damage Research Product Guide
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