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 public 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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