PID-34 | PID-34 : Covalent Degrader (PROTAC) of PIN1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Selectivity
In Vivo
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIN1
    • DC50:177 nM
    • Dmax:95%
    Covalent
    10 µM

    Selectivity

    Potency
    Cellular
    In Vitro

    PIN1

    Mode of Action: Covalent

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1039/d3sc06558h

    Negative Control Compounds

    canSAR7437547
    Notes: Negative controls P1D-34N1 bearing a methyl group in glutarimide NH to reduce its binding affinity to CRBN
    canSAR7437566
    Notes: P1D-34N2 is non-covalent and reduce its binding affinity to Pin1, resulting in a very weak effect on the levels of Pin1 protein.

    Chemical Information

    Molecular Formula C40H59ClN6O9S
    SMILEs CC(C)(CNC(=O)CCC(=O)NCCCCCCCCCCCCNc1ccc2c(c1)C(=O)N(C1CCC(=O)NC1=O)C2=O)CN(C(=O)CCl)C1CCS(=O)(=O)C1
    InChI InChI=1S/C40H59ClN6O9S/c1-40(2,27-46(36(51)24-41)29-19-22-57(55,56)25-29)26-44-34(49)18-17-33(48)43-21-12-10-8-6-4-3-5-7-9-11-20-42-28-13-14-30-31(23-28)39(54)47(38(30)53)32-15-16-35(50)45-37(32)52/h13-14,23,29,32,42H,3-12,15-22,24-27H2,1-2H3,(H,43,48)(H,44,49)(H,45,50,52)
    Molecular weight 834.38 Da
    AlogP 3.6940000000000035
    HBond acceptors 15
    HBond donors 4
    Atoms 116

    References

    Publications

    Cross References

    Expert Reviews


    (on 30 Oct 2024 )
    Cellular Use Rating
    In this paper, P1D-34 (the covalent Pin1 inhibitor Sulfopin linked to a cereblon ligand), induced potent Pin1 degradation with a DC50 value of 177 nM. The cellular IC50 varies between cells but is around...
    (on 2 Dec 2024 )
    Cellular Use Rating
    While the authors have shown that PID-34 degrades PIN1 in the cellular setting, and that this is consistent with the expected mechanism for a PROTAC (proper mechanistic studies in the presence of neddylation...
    (on 6 Feb 2026 )
    Cellular Use Rating
    Limited data is provided to support the use of this degrader as chemical probe and the presented data requires further validation or re-analysis. Although a negative control is presented, Western Blot...
    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