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PF 4800567
- Soluble in DMSO
- MF: C17H18ClN5O2
- MW: 359.81
Description
PF 4800567 is a potent and selective casein kinase 1ε (CK1ε/CSNK1E) inhibitor with an IC50 value of 32 nM and more than 20-fold selectivity over CK1δ.
CK1ε regulates circadian clock proteins, phosphorylation-dependent signaling and cellular pathway timing. PF 4800567 is useful for dissecting CK1ε-dependent biology while minimizing cross-inhibition of the closely related CK1δ isoform.
Key Features
- Potent CK1ε/CSNK1E inhibitor
- IC50: 32 nM for CK1ε
- More than 20-fold selective over CK1δ
- Useful probe for circadian and phosphorylation-dependent signaling
Applications
- CK1ε kinase pharmacology
- Circadian rhythm and PER protein phosphorylation studies
- Kinase selectivity and cellular pathway profiling
- Casein kinase signaling assay development
More Information
| Parent CAS No. | 1188296-52-7 |
|---|---|
| Chemical Name | 3-((3-chlorophenoxy)methyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine |
| SMILES | C1=NC(N)=C2C(COC3=CC=CC(Cl)=C3)=NN(C3CCOCC3)C2=N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C17H18ClN5O2/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21) |
| InChiKey | AUMDBEHGJRZSOO-UHFFFAOYSA-N |
| CID | 53472153 |
| Short Description | CK 1e inhibitor |
References
- KM Walton et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J. Pharmacol. Exp. Ther. 2009, 330(2), 430-439.
- QJ Meng et al. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proc. Natl. Acad. Sci. USA. 2010, 107(34), 15240-15245.
- CD Bryant et al. Csnk1e is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids. Neuropsychopharmacology. 2011, 37, 1026-1035.
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