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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
    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 2.8992000000000013
    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 public comments)
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