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PF-367 | PF-367 : Inhibitor of GSK3A, GSK3B
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GSK3A
  • IC50:10 nM
    GSK3B
    • IC50:9.0 nM
    • IC50:1.1 nM
    • IC50:2.1 nM
    • IC50:466 nM
    Inhibitor
    up to 5 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    PF-367 was screened against a broad panel of 240 kinases in biochemical functional assays at a conce ...

    Potency
    Cellular
    In Vitro

    GSK3A

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1002/anie.201603797

    GSK3B

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1002/anie.201603797

    In Vivo Validations

    Rat
    Dose: 50 mg/Kg
    Route of delivery: Intravenous
    Target engagement assay: PF-367 showed a rapid 76 % reduction of P-tau levels in the brain and 92 % reduction of phospho-glycogen synthase (pGS) in skeletal muscle after one hour of administration in rats

    DOI Reference: 10.1002/anie.201603797

    Chemical Information

    Molecular Formula C16H16ClN5O3
    SMILEs COc1ccc(-c2ocnc2C(=O)NCCCn2cncn2)cc1Cl
    InChI InChI=1S/C16H16ClN5O3/c1-24-13-4-3-11(7-12(13)17)15-14(20-10-25-15)16(23)19-5-2-6-22-9-18-8-21-22/h3-4,7-10H,2,5-6H2,1H3,(H,19,23)
    Molecular weight 361.09 Da
    AlogP 2.4152000000000005
    HBond acceptors 8
    HBond donors 1
    Atoms 41

    References

    Publications

    Cross References

    canSARChEMBLBindingDBPDB

    Vendors

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    Expert Reviews

    by SERP
    (on 7 Feb 2023)
    Cellular Use Rating
    In Model Organisms
    The compound is effective at inhibiting tau phosphorylation in rat brain. However, "the short in vivo half-life of PF-367 precluded any long-term chronic behavioral studies and kinetics of PF-367 binding...
    by SERP
    (on 21 Feb 2023)
    Cellular Use Rating
    In Model Organisms
    (The reviewer did not leave any public comments)
    by SERP
    (on 27 Feb 2023)
    Cellular Use Rating
    In Model Organisms
    Rat is a suitable in vivo model, but the short in vivo half-life of PF-367 will prevent long-term chronic studies
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria