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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

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 public 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 public comments)
by SERP
(on 17 Apr 2017)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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