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BAZ2-ICR | BAZ2-ICR : Antagonist of BAZ2A and 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:109 nM
  • IC 50:130 nM
BAZ2B
  • Kd:170 nM
  • IC 50:180 nM
Antagonist
500 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: Kd - 1.55 uM

Potency Assay Off-Target:
CEREP, Thermal Shift Assay
Selectivity Assessment Description:
In Cerep screen of 55 receptors, BAZ2-ICR had a clean off-target profile. In thermal shift assay of ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In FRAP assay, BAZ2-ICR did not displace BRD4 from chromatin.
Selectivity Assessment Description:
In FRAP assay, BAZ2-ICR did not displace BRD4 from chromatin.

Potency
Cellular
In Vitro

BAZ2A

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm501963e

BAZ2B

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm501963e

In Vivo Validations

Mouse
Dose: 5 mg/kg
Route of delivery: Intravenous, Oral
Plasma half life: 0.93 h (IV), 0.90 h (oral)
Systemic clearance: 36.2 mL/min/kg (IV), 36.0 mL/min/kg (oral)

DOI Reference: 10.1021/jm501963e

Orthogonal Probes def

GSK2801

Chemical Information

Molecular Formula C20H19N7
SMILEs Cn1cc(CCn2cnc(-c3cnn(C)c3)c2-c2ccc(C#N)cc2)cn1
InChI InChI=1S/C20H19N7/c1-25-12-16(10-23-25)7-8-27-14-22-19(18-11-24-26(2)13-18)20(27)17-5-3-15(9-21)4-6-17/h3-6,10-14H,7-8H2,1-2H3
Molecular weight 357.17 Da
AlogP 2.7984800000000014
HBond acceptors 7
HBond donors --
Atoms 46

References

Publications

Cross References

Vendors

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Expert Reviews

by SERP
(on 15 Aug 2016 )
Cellular Use Rating
BAZ2A/B (bromodomain adjacent to zinc finger domain, 2A/B) is a member of the nuclear remodeling complex (NoRC), but little is known about the function. Elevated levels of BAZ2A expression are observed...
by SERP
(on 24 Oct 2016 )
Cellular Use Rating
In Model Organisms
In cells, the probe shows good selectivity, but the compound has only a moderate binding affinity ~100 nM and cellular activity (1 µM in FRAP assay). BAZ2-ICR has been shown by ITC to bind to BAZ2A...
by SERP
(on 15 Jun 2017 )
Cellular Use Rating
In Model Organisms
This probe has modest affinity to BZA2A (130 nM) and BZA2B (180 nM). It has good selectivity against 45 other bromodomains with the exception of CERC2 against which BAZ2-ICR is only 10-15 fold selective....
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