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GSK2801 | Antagonist of BAZ2A, BAZ2B
RATINGS:
Cellular Use: (3 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
BAZ2A
  • Kd:257 nM
  • IC 50:400 nM
BAZ2B
  • Kd:136 nM
  • IC 50:430 nM
Antagonist
1 uM

Selectivity

In Vitro Selectivity Assessment
TAF1L

Gene ID: Q8IZX4

Organism: Homo sapiens

Family: TAF1 family

Potency: IC 50 - 320 nM

Potency Assay Off-Target:
Thermal stability assays.
Selectivity Assessment Description:
42 Bromodomains tested, GSK2801 was only active against BRD9 1.1 uM and TAF1L 0.32 uM

Potency
Cellular
In Vitro

BAZ2A

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b00209

BAZ2B

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b00209

In Vivo Validations

Mouse
Dose: 30 mg/kg
Route of delivery: Intraperitoneal, Oral
Plasma half life: 4.5 h (IP), 1.5 h (oral)

DOI Reference: 10.1021/acs.jmedchem.5b00209

Negative Control Compounds

GSK8573, with activity against BRD9

Orthogonal Probes def

BAZ2-ICR

Chemical Information

Molecular Formula C20H21NO4S
SMILEs CCCOc1ccn2c(C(C)=O)cc(-c3ccccc3S(C)(=O)=O)c2c1
InChI InChI=1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3,23)24/h5-10,12-13H,4,11H2,1-3H3
Molecular weight 371.12 Da
AlogP 4.001200000000003
HBond acceptors 5
HBond donors --
Atoms 47

References

Publications

Cross References

Expert Reviews

by SERP
(on 10 Aug 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 10 Aug 2016 )
Cellular Use Rating
In Model Organisms
GSK2801 PK parameters after IP/oral dosing in male CD1 mice suggest it has potential as in vivo probe, especially if applied side-by-side with structurally similar, negative control.
by SERP
(on 1 Feb 2017 )
Cellular Use Rating
In Model Organisms
GSK2801 is a useful probe for BAZ2A and BAZ2B bromodomains. While it has encouraging selectivity relative to other bromodomains, the utility GSK2801 is somewhat limited by weak potency, requiring it...
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