Chemical Probes logo
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
Download

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

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    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 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