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PF-670462
Cat No.
CEI-1476
Product Overview
PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 80 nM and 13 nM, respectively. CK1ε and CK1δ belong to the casein kinase 1 family which is serine/threonine-selective enzyme and plays an important role in regulating circadian rhythm. In COS-7 cells cotransfected with GFP-tagged PER3 and the human CK1ε enzyme, PF-670462 inhibited PER3 nuclear translocation in a concentration-dependent way. In primary lung fibroblast cells obtained from WT mice, PF-670462 significantly lengthened the circadian period in a dose-dependent way. And with a dose of 1 μM, the period in WT fibroblast cells extended to 33 h. In WT, Ck1ε −/−and Ck1ε tau mice, PF-670462 (10 mg/kg/d) significantly lengthened the period of activity rhythms in all three genotypes (WT: 0.44 h, Ck1ε tau: 0.39 h, Ck1ε −/−: 0.42 h). In WT mice, the activity onset occurred 10.4 h after 24 d of treatment. Also, PF-670462 caused identical period lengthening in WT and Ck1ε −/−mice, which suggested that the effect of CK1δ on the circadian period.
CAS No.
950912-80-8
Molecular Weight
410.32
Purity
0.9958
Storage
Store at -20°C
Synonyms
PF 670462; PF670462
Targets
CK1 ε/δ
Molecular Formula
C19H22Cl2FN5
Chemical Name
4-[3-cyclohexyl-5-(4-fluorophenyl)imidazol-4-yl]pyrimidin-2-amine; dihydrochloride
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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