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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
  • IC50:6.3 nM
  • Kd:2 nM
  • IC50:250 nM
  • IC50:250 nM
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

DOI Reference: 10.1021/acs.jmedchem.9b02071

In Vivo Validations

Rat
Dose: 2.9 mg/kg
Route of delivery: Intravenous
Plasma half life: 7.7 h
Systemic clearance: 21 mL/min/kg
Area Under the Curve:: 6.2 μM·h
Volume of Distribution at Steady-State: 0.72 L/kg

DOI Reference: 10.1021/acs.jmedchem.9b02071

Dose: 33 mg/Kg
Route of delivery: Oral
Plasma half life: 6.4 h
Cmax: 2.9 uM
Tmax: 1.0 h
Area Under the Curve:: 13 μM·h
Bioavailability: 18%
Target engagement assay: HPMC (suspension) (mean ± SD)

DOI Reference: 10.1021/acs.jmedchem.9b02071

Dose: 31 mg/Kg
Route of delivery: Oral
Plasma half life: 6.0 h
Cmax: 14 uM
Tmax: 1.0 h
Area Under the Curve:: 38 μM·h
Bioavailability: 56%
Target engagement assay: PEG400/Solutol HS-15/water (solution) (mean ± SD)

DOI Reference: 10.1021/acs.jmedchem.9b02071

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

Vendors

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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