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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

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Targets Biochemical/Biophysical Potency Cellular Potency
BAZ2A
  • Kd:257 nM
  • IC 50:400 nM
BAZ2B
  • Kd:136 nM
  • IC 50:430 nM
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

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

Expert Reviews

by SERP
(on 10 Aug 2016)
Cellular Use Rating
(The reviewer did not leave any public 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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