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PF-9363 | PF-9363 : Inhibitor of KAT6A, KAT6B
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
KAT6A
  • Ki:0.27 nM
  • IC50:0.85 nM
  • IC50:370 nM
KAT6B
  • Ki:2.4 nM
    Inhibitor
    100 - 300 nM
    up to 1 uM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    CTx-648 growth inhibitory activity was tested in a panel of 60 breast cancer cell lines
    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selective within target family: KAT7 (Ki 70 nM), KAT5 (Ki 420 nM) and KAT8 (Ki 670 nM)

    Potency
    Cellular
    In Vitro

    KAT6A

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2023.07.005

    KAT6B

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1016/j.chembiol.2023.07.005

    In Vivo Validations

    Mouse
    Dose: 1.0 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 18 h
    Systemic clearance: 0.085 mL/min/Kg
    Volume of Distribution at Steady-State: 0.12 L/Kg

    DOI Reference: 10.1016/j.chembiol.2023.07.005

    Dose: 1 mg/Kg
    Route of delivery: Oral
    Bioavailability: 92%

    DOI Reference: 10.1016/j.chembiol.2023.07.005

    Negative Control Compounds

    Ctx-533
    Notes: Ctx-533 appears inactive in cellular assays with Ki 500 nM in Biochemical assay
    SMILES: COC1=CC=C(Cl)C=C1S(=O)(NC2=NOC3=C2C(OC)=CC=C3)=O

    Chemical Information

    Molecular Formula C20H20N4O6S
    SMILEs COc1cccc(OC)c1S(=O)(=O)Nc1noc2cc(Cn3cccn3)cc(OC)c12
    InChI InChI=1S/C20H20N4O6S/c1-27-14-6-4-7-15(28-2)19(14)31(25,26)23-20-18-16(29-3)10-13(11-17(18)30-22-20)12-24-9-5-8-21-24/h4-11H,12H2,1-3H3,(H,22,23)
    Molecular weight 444.11 Da
    AlogP 0.0
    HBond acceptors 10
    HBond donors 1
    Atoms 51

    Vendors

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

    Expert Reviews

    by SERP
    (on 12 Oct 2023 )
    Cellular Use Rating
    In Model Organisms
    This is a good probe for this family of proteins.
    by SERP
    (on 17 Oct 2023 )
    Cellular Use Rating
    In Model Organisms
    PF-9363 is a quality chemical probe for KAT6A/6B with exquisite potency and mouse PK. The overall selectivity is difficult to judge; KAT6B/KAT7 appears to be 29x based on binding and cellular selectivity...
    by SERP
    (on 27 Oct 2023 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    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