Biological Activity
Selective casein kinase 1ε inhibitor; displays 22-fold greater potency towards CK1ε than CK1δ (IC50 values are 32 and 711 nM for CK1ε and CK1δ respectively). ATP competitive. Displays minimal effect on the circadian clock.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 4800567 is reviewed on the chemical probes website.
Compound Libraries
PF 4800567 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 396.27 |
| Formula | C17H18ClN5O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1391052-28-0 |
| PubChem ID | 71751553 |
| InChI Key | QZXZQMUZEHTFHD-UHFFFAOYSA-N |
| Smiles | NC1=C(C(COC4=CC(Cl)=CC=C4)=NN2C3CCOCC3)C2=NC=N1.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 | 39.63 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 396.27. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.52 mL | 12.62 mL | 25.24 mL |
| 5 mM | 0.5 mL | 2.52 mL | 5.05 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Walton et al (2009) Selective inhibition of casein kinase 1ε minimally alters circadian clock period. J.Pharmacol.Exp.Ther. 330 430 PMID: 19458106
Etchegaray et al (2010) Casein kinase 1 delta (CK1δ) regulates period length of the mouse suprachiasmatic circadian clock in vitro. PLoS One 5 e10303 PMID: 20421981
Meng et al (2010) Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proc.Natl.Acad.Sci.USA 107 15240 PMID: 20696890
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