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Submit ReviewPF 4800567 hydrochloride
Description: Selective casein kinase 1ε inhibitor
Chemical Name: 3-[(3-Chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for PF 4800567 hydrochloride
PF 4800567 hydrochloride is a 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 for PF 4800567 hydrochloride
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 for PF 4800567 hydrochloride
PF 4800567 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PF 4800567 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PF 4800567 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.63 | 100 |
Preparing Stock Solutions for PF 4800567 hydrochloride
The following data is based on the product molecular weight 396.27. 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 | 2.52 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 for PF 4800567 hydrochloride
References for PF 4800567 hydrochloride
References are publications that support the biological activity of the product.
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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5 Citations for PF 4800567 hydrochloride
Citations are publications that use Tocris products. Selected citations for PF 4800567 hydrochloride include:
Zhang et al (2013) Dissociation of circadian and circatidal timekeeping in the marine crustacean Eurydice pulchra. Curr Biol 23 1863 PMID: 24076244
Oren et al (2015) Profiling molecular and behavioral circadian rhythms in the non-symbiotic sea anemone Nematostella vectensis. Mol Biol Cell 5 11418 PMID: 26081482
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
Cheong et al (2015) Casein kinase 1α-dependent feedback loop controls autophagy in RAS-driven cancers. J Clin Invest 125 1401 PMID: 25798617
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
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