PF-4800567 is a selective, ATP competitive casein kinase 1ε inhibitor with IC50 values of 32 and 711 nM for CK1ε and CK1δ respectively. Casein kinase 1 epsilon (CK1epsilon) and casein kinase 1 delta (CK1delta) are closely related Ser-Thr protein kinases that serve as key clock regulators as demonstrated by mammalian mutations in each that dramatically alter the circadian period. PF-4800567 displays 22-fold greater potency towards CK1ε than CK1δ. PF-4800567 completely blocks CK1epsilon-mediated PER3 nuclear localization and PER2 degradation.
Cell Experiment | |
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Cell lines | COS-7 cells |
Preparation method | Nuclear Translocation. CK1ϵ- and CK1δ-dependent PER3 nuclear translocation was run as described previously for CK1ϵ (Badura et al., 2007), with alterations as indicated below. CK1δ-dependent PER3 nuclear translocation was performed with human full-length CKIδ-pcDNA4/HisA cotransfected into COS-7 cells with the GFP-tagged murine PER3. The sensitivity of the assay was increased by incorporating an anti-GFP antibody-staining step. After the plates were fixed with 4% paraformaldehyde and washed in PBS, cells were blocked and permeabilized in PBS with 4% goat serum and 0.1% Triton X-100 for 1 h at room temperature. Blocking buffer was then replaced with a polyclonal anti-GFP antibody (Invitrogen), diluted 1:1000 in blocking buffer, and incubated for 2 h. After three washes in PBS, goat anti-rabbit Alexa Fluor 488 secondary antibody (Invitrogen), diluted 1:1000 in Hoechst staining solution, was added and incubated for 1 h before three final washes in PBS. |
Concentrations | 0, 0.01, 0.1, 1, 10μM |
Incubation time | 1~2 hr |
Animal Experiment | |
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Animal models | C57BL/6J mice |
Formulation | 20% hydroxypropyl β-cyclodextrin |
Dosages | 100 mg/kg daily for 3 days |
Administration | s.c. |
Molecular Weight | 359.81 |
Formula | C17H18ClN5O2 |
CAS Number | 1188296-52-7 |
Solubility (25°C) | DMSO ≥30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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