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PF-4800567

Cat. No. M1903
PF-4800567 Structure
Size Price Availability
5mg USD 82 Custom Synthesis
10mg USD 145 Custom Synthesis
50mg USD 490 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
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
Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 359.81
Formula C17H18ClN5O2
CAS Number 1188296-52-7
Purity >98%
Solubility DMSO ≥30 mg/mL
Storage at -20°C
References

Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.
Walton KM, et al. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9. PMID: 19458106.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-4800567 supplier, Casein Kinase, inhibitors

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