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WM-1119 | WM-1119 : Inhibitor of KAT6A
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
  • IC50, KD:6.3 nM IC50, 2 nM KD
  • IC50:0.250 uM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
WM-1119 is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7
In Cell Selectivity Assessment
Selectivity Assessment Description:
No affinity on off-target panel of 159 diverse targets at 1 or 10 µM

Potency
Cellular
In Vitro

KAT6A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

In Vivo Validations

Rat
Dose: 2.9 (IV) mg/kg, 33 (PO) mg/kg
Route of delivery: Intravenous, Oral
Plasma half life: 7.7 h (IV), 6.4 h (PO)
Systemic clearance: 21 mL/min/kg

Reference: --

Negative Control Compounds

WM-2474
Notes: WM-2474: KAT6A IC50 > 50 µM (HAT activity assay (AlphaScreen)); No effect on Fucci MEFs at 10 µM. Clean GPCR scan.

Chemical Information

Molecular Formula C18H13F2N3O3S
SMILEs O=C(NNS(=O)(=O)c1ccccc1F)c1cc(F)cc(-c2ccccn2)c1
InChI InChI=1S/C18H13F2N3O3S/c19-14-10-12(16-6-3-4-8-21-16)9-13(11-14)18(24)22-23-27(25,26)17-7-2-1-5-15(17)20/h1-11,23H,(H,22,24)
Molecular weight 389.06 Da
AlogP 2.6501
HBond acceptors 6
HBond donors 2
Atoms 40

References

Publications

    Cross References

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    Expert Reviews

    by SERP
    (on 28 Aug 2020 )
    Cellular Use Rating
    In Model Organisms
    This probe has been developed by a strong medicinal chemistry approach for which more than 180 analogs have been profiled in in vitro KAT6A activity assays (Priebbenow J Med Chem 2020). WM-1119 is a...
    by SERP
    (on 24 Sept 2020 )
    Cellular Use Rating
    In Model Organisms
    I agree with the recommended oral dose in rats, however I do not recommend dosing rats intravenously with WM-1119. In mice, I recommend dosing intraperitoneally at 50mg/kg
    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