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PT-65 | PT-65 : Degrader (PROTAC) of GSK3A, GSK3B
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GSK3A
    • DC50:28.3 nM
    • Dmax:94.3 ± 2.2%
    GSK3B
    • Kd:12.41 nM
    • DC50:34.2 nM
    • Dmax:90.8 ± 2.9%
    Degrader (PROTAC)
    up to 500 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    The selectivity of PT-65 was evaluated by the global proteome analysis using tandem mass tag (TMT)-b ...

    Potency
    Cellular
    In Vitro

    GSK3A

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.ejmech.2021.113889

    GSK3B

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.ejmech.2021.113889

    Chemical Information

    Molecular Formula C51H63N13O12S
    SMILEs Nc1ncc(-c2ccc(S(=O)(=O)N3CCN(CCCCc4cn(CCOCCOCCOCCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)nn4)CC3)cc2)nc1C(=O)Nc1cccnc1
    InChI InChI=1S/C51H63N13O12S/c52-47-46(49(67)56-37-6-4-15-53-33-37)57-42(34-55-47)36-9-11-39(12-10-36)77(70,71)63-20-18-61(19-21-63)17-2-1-5-38-35-62(60-59-38)22-24-73-26-28-75-30-32-76-31-29-74-27-25-72-23-16-54-41-8-3-7-40-45(41)51(69)64(50(40)68)43-13-14-44(65)58-48(43)66/h3-4,6-12,15,33-35,43,54H,1-2,5,13-14,16-32H2,(H2,52,55)(H,56,67)(H,58,65,66)
    Molecular weight 1081.44 Da
    AlogP 0.0
    HBond acceptors 25
    HBond donors 5
    Atoms 140

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

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    Expert Reviews

    by SERP
    (on 18 May 2023)
    Cellular Use Rating
    The proteomics for this compound was done in singlicate (and the raw data is not available), so there is no P-values/fold change information available. I, therefore, think it will not be possible to adequately...
    by SERP
    (on 19 May 2023)
    Cellular Use Rating
    This molecule can potently degrade with GSK3a and GSK3b with a relatively rapid degradation profile at 1uM in SHSY5Y cells. Adequate controls are provided to demonstrate proteasomal dependence and competition...
    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