WM-3835 | WM-3835 : Inhibitor of KAT7
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KAT7
  • IC50:30 nM
  • Kd:34 nM
  • IC50:297 nM
Inhibitor
Concentration in cells may need to be higher than 3 uM in certain experiments, and users should confirm sufficient efficacy in their models.
3 uM

Selectivity

In Vitro Selectivity Assessment
KAT6A

Gene ID: Q92794

Organism: Homo sapiens

Family: MYST (SAS/MOZ) family

Potency: IC50 - 17 nM

Selectivity Assessment Description:
biochemical assay and SPR (Kd = 7 nM)

Potency
Cellular
In Vitro

KAT7

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41586-019-1835-6

In Vivo Validations

Mouse
Dose: 100 mg/Kg BID
Route of delivery: Oral
Plasma half life: 5 min
Systemic clearance: ~400 uL/min/mg protein
Fb : 99.8%

DOI Reference: 10.1038/s41586-019-1835-6

Negative Control Compounds

WM-2474

Chemical Information

Molecular Formula C20H17FN2O4S
SMILEs Cc1cc(-c2ccccc2)cc(C(=O)NNS(=O)(=O)c2cccc(O)c2)c1F
InChI InChI=1S/C20H17FN2O4S/c1-13-10-15(14-6-3-2-4-7-14)11-18(19(13)21)20(25)22-23-28(26,27)17-9-5-8-16(24)12-17/h2-12,23-24H,1H3,(H,22,25)
Molecular weight 400.09 Da
AlogP 3.13002
HBond acceptors 6
HBond donors 3
Atoms 45

References

Cross References

Vendors

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Expert Reviews


(on 22 Feb 2022 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
(on 26 Feb 2022 )
Cellular Use Rating
In Model Organisms
WM-3835 is an excellent chemical probe for HBO1. It should be used alongside its inactive control analog, WM-2474, whenever possible. Strengths of validation data include its robust SAR, nanomolar biochemical...
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