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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.
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Source | Oncogene (2011). Figure 5. PF-4800567 |
| Method | cell proliferation assay | |
| Cell Lines | HEK293 and HT1080 cell | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | We confirmed that PF480 selectively inhibited CK1ɛ using the in vivo autophosphorylation assay. PF480 was less effective than PF670 at inhibition of Wnt/β-catenin signaling |
| Cell Experiment | |
|---|---|
| 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 | |
|---|---|
| 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 |
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| (R)-DRF053 dihydrochloride
(R)-DRF053 dihydrochloride is a potent inhibitor of casein kinase 1 (CK1), CDK1/cyclin B, and CDK5/p25, with IC50s of 14 nM, 220 nM, and 80 nM, respectively.(R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cellular models. In addition, (R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cell models. |
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