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CZH-Z16 | CZH-Z16 : Degrader (PROTAC) of HDAC8
RATINGS:
Cellular Use: (3 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
HDAC8
    • DC50:0.32 nM
    • DC50:2.4 nM
    • DC50:3.1 nM,
    • DC50:0.27 nM
    Degrader (PROTAC)
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selectivity within family: Z16 shows very little inhibitory activity agains the HDAC family HDAC1 I ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    No obvious HDAC1, HDAC2, HDAC3, HDAC4, HDAC6, HDAC7, and HDAC11 degradation was observed on Western ...

    Potency
    Cellular
    In Vitro

    HDAC8

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.4c00836

    Negative Control Compounds

    NC-Z16
    Notes: NC-Z16 showed over 6-fold decreased HDAC8 binding affinity (HDAC8 inhibition IC50 = 16.6 μM).
    canSAR7369919
    Notes: cpd 32 did not induce HDAC8 degradation

    Chemical Information

    Molecular Formula C32H44N6O4
    SMILEs CCCCCCNNC(=O)c1ccc(CNC(=O)CN2CCC(c3ccc(NC4CCC(=O)NC4=O)cc3)CC2)cc1
    InChI InChI=1S/C32H44N6O4/c1-2-3-4-5-18-34-37-31(41)26-8-6-23(7-9-26)21-33-30(40)22-38-19-16-25(17-20-38)24-10-12-27(13-11-24)35-28-14-15-29(39)36-32(28)42/h6-13,25,28,34-35H,2-5,14-22H2,1H3,(H,33,40)(H,37,41)(H,36,39,42)
    Molecular weight 576.34 Da
    AlogP 3.2142000000000017
    HBond acceptors 10
    HBond donors 5
    Atoms 86

    References

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    Expert Reviews

    by SERP
    (on 6 Nov 2024 )
    Cellular Use Rating
    The cellular effects on biological pathways is ~3logs weaker than the degradation effects in the same cells. No proteomics data (and few other data) are supplied to show that the cell biology is only derived...
    by SERP
    (on 25 Nov 2024 )
    Cellular Use Rating
    This compound is among the most potent HDAC8 degraders currently available. A limitation for full recommendation as a cellular probe for HDAC8 is the current lack of global proteomics data to confirm selectivity...
    by SERP+
    (on 6 Feb 2026 )
    Cellular Use Rating
    This degrader lacks robust selectivity data, i.e. no proteomic data are shown, and selectivity has only been assessed against other Class I HDACs. While selectivity is shown through Western Blots within...
    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