A selective CK1ε inhibitor
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PF-4800567

Item No. 19171

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(3-chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS Number
1188296-52-7
Molecular Formula
C17H18ClN5O2
Formula Weight
359.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 1 mg/ml
λmax
273 nm
SMILES
ClC1=CC(OCC2=NN(C3CCOCC3)C4=NC=NC(N)=C42)=CC=C1
InChi Code
InChI=1S/C17H18ClN5O2/c18-11-2-1-3-13(8-11)25-9-14-15-16(19)20-10-21-17(15)23(22-14)12-4-6-24-7-5-12/h1-3,8,10,12H,4-7,9H2,(H2,19,20,21)
InChi Key
AUMDBEHGJRZSOO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $157

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    10 mg

    $255

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    25 mg

    $583

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    Product Description

    PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.1 It blocks CK1ε-mediated PER3 nuclear localization and PER2 degradation, both of which are proteins important for maintaining circadian rhythms in cells.1 PF-4800567 has been used in the study of the CK1 enzymes in the regulation of circadian rhythm and is also reported to have neuroprotective effects.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Walton, K.M., Fisher, K., Rubitski, D., et al. Selective inhibition of casein kinase 1ε minimally alters circadian clock period. J. Pharmacol. Exp. Ther. 330(2), 430-439 (2009).

    2. Meng, Q.J., Maywood, E.S., Bechtold, D.A., et al. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proc. Natl. Acad. Sci. USA 107(34), 15240-15245 (2016).

    3. Perez, D.I., Gil, C., and Martinez, A. Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases. Med. Res. Rev. 31(6), 924-954 (2011).