PF 670462

Pricing Availability Delivery Time Qty
Cat.No. 3316 - PF 670462 | C19H20FN5.2HCl | CAS No. 950912-80-8
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)
Datasheet
Citations (7)
Literature

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.

Compound Libraries

PF 670462 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.03 100
ethanol 20.52 50
water 41.03 100

Preparing Stock Solutions

The following data is based on the product molecular weight 410.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

References

References are publications that support the products' biological activity.

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 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


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View all Casein Kinase 1 Inhibitors

Keywords: Potent selective CK1ε CK1epsilon CK1δ CK1delta inhibitors inhibits Casein Kinases 1 PF670462 circadian rhythms Casein Kinase 1

7 Citations for PF 670462

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

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

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

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

Zantke et al (2013) Circadian and circalunar clock interactions in a marine annelid. PLoS One 5 99 PMID: 24075994

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


Do you know of a great paper that uses PF 670462 from Tocris? If so please let us know.

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