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Chemical Structure| 1188296-52-7 Chemical Structure| 1188296-52-7

Structure of PF-4800567
CAS No.: 1188296-52-7

Chemical Structure| 1188296-52-7

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CAS No.: 1188296-52-7

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PF-4800567 is an inhibitor of casein kinase 1ε (CK1ε) with IC50 of 32 nM.

Synonyms: PF-4800567

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Product Details of PF-4800567

CAS No. :1188296-52-7
Formula : C17H18ClN5O2
M.W : 359.81
SMILES Code : NC1=C2C(N(C3CCOCC3)N=C2COC4=CC=CC(Cl)=C4)=NC=N1
Synonyms :
PF-4800567
MDL No. :MFCD22123245
InChI Key :AUMDBEHGJRZSOO-UHFFFAOYSA-N
Pubchem ID :53472153

Safety of PF-4800567

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PF-4800567

DNA
Hedgehog

Isoform Comparison

Biological Activity

Target
  • CK1

    casein kinase 1 epsilon, IC50:32 nM

    casein kinase 1 delta, IC50:711 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Ck1ε−/− SCN slices 1 μM no significant effect on circadian period PMC2930590
Ck1εtau SCN slices 1 μM significant lengthening of circadian period PMC2930590
WT SCN slices 1 μM no significant effect on circadian period PMC2930590
Ck1ε−/− lung fibroblasts 1 μM no significant lengthening of circadian period (0.3 ±0.3 h) PMC2930590
Ck1εtau mutant lung fibroblasts 1 μM slight lengthening of circadian period PMC2930590
WT lung fibroblasts 1 μM slight lengthening of circadian period (0.9 ±0.13 h), but no significant effect in Ck1ε−/− cells (0.3 ±0.3 h) PMC2930590
HT1080 cells 1 μM 7 days Test the effect of PF4800567 on cell proliferation PMC3109269
HEK293 cells 1 μM 7 days Test the effect of PF4800567 on cell proliferation PMC3109269
HEK293STF3A cells 1 μM 16 h Test the inhibitory effect of PF4800567 on Wnt/β-catenin signaling PMC3109269
HEK293STF3A cells 1 μM 30 min Test the inhibitory effect of PF4800567 on CK1ε autophosphorylation PMC3109269
Mouse suprachiasmatic nucleus (SCN) organotypic slice cultures 0.5 μM 5 cycles By inhibiting CK1ε activity, the short period of CK1εTau/Tau mutant was restored to the wild-type 24 h period, revealing the critical role of CK1ε in the SCN clock. PMC5013184
U87MG cells 28.4 μM PF-4800567 had a modest effect on the viability of U87MG cells with an IC50 of approximately 28.4 μM PMC6134061

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice WT, Ck1εtau mutant, and Ck1ε−/− mice Subcutaneous injection 100 mg/kg Daily injections for 10 days No significant effect on the period or phase of behavioral rhythms in WT or Ck1ε?/? mice, but significant period lengthening in Ck1εtau mutant mice PMC2930590
Mice B6.B6Csnk1e and B6.D2Csnk1e mice Intraperitoneal injection 40 mg/kg Single administration PF-4800567 increased methamphetamine- and fentanyl-induced locomotor activity PMC3280656

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.90mL

2.78mL

1.39mL

27.79mL

5.56mL

2.78mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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