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GSK4027 | Antagonist of KAT2B, KAT2A
RATINGS:
Cellular Use: (5 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
KAT2B
  • Ki:1.25 nM
  • IC 50:60 nM
KAT2A
  • IC 50:40 nM
  • Ki:1.25 nM
  • IC 50:63 nM
  • IC 50:60 nM
Antagonist
50 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - BRPF3: 100 nM, BRD1: 110 nM, FALZ: 130 nM, BRPF1: 140 nM

Potency Assay Off-Target:
BROMOscan assay run at DiscoverX. In the assay, PCAF and GCN5: Ki=1.4 nM, hence >70 fold window to ...
Selectivity Assessment Description:
BROMOscan assay run at DiscoverX. In the assay, PCAF and GCN5: Ki=1.4 nM, hence >70 fold window to o ...

Potency
Cellular
In Vitro

KAT2B

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.6b01566

KAT2A

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.6b01566

Negative Control Compounds

GSK4028

Orthogonal Probes def

L-Moses

Chemical Information

Molecular Formula C17H21BrN4O
SMILEs CN1C[C@H](Nc2cnn(C)c(=O)c2Br)C[C@H](c2ccccc2)C1
InChI InChI=1S/C17H21BrN4O/c1-21-10-13(12-6-4-3-5-7-12)8-14(11-21)20-15-9-19-22(2)17(23)16(15)18/h3-7,9,13-14,20H,8,10-11H2,1-2H3/t13-,14+/m0/s1
Molecular weight 376.09 Da
AlogP 2.4425999999999997
HBond acceptors 5
HBond donors 1
Atoms 44

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 17 Mar 2017 )
Cellular Use Rating
GSK4027 is a potent inhibitor of the bromodomain of PCAF and GCN5 with good selectivity over other BRD-containing proteins. GSK4027 has good aqueous solubility, cell permeability, and it shows cellular...
by SERP
(on 27 Mar 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 10 Apr 2017 )
Cellular Use Rating
In Model Organisms
GSK4027 represents an orthogonal method to inhibit binding of the bromodomains present in PCAF and GCN5 to their targets compared with L-Moses. This compound shows similar in vitro and cellular potency...
by SERP
(on 17 Apr 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 17 Apr 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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