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BTZO-1 | ARE Activator of MIF
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (1 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
MIF
  • Kd:68.6 nM
  • Kd:147 nM
  • MEC1.5, MEC2.0:MEC1.5 16 nM
up to 1 uM

Selectivity

Potency
Cellular
In Vitro

MIF

Mode of Action: ARE Activator

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2010.10.011

Negative Control Compounds

BTZO-4
Notes: ARE-Luc Reporter Assay (Activation of ARE (antioxidant response element)-mediated cytoprotective gene expression): MEC2.0 > 10 µM; Apoptosis inhibition: MEC1.5 > 1 µM; Clean GPCR scan KINOMEScan with 468 targets at 1 µM: Closest off-targets of primary data (% Ctrl) is EIF2AK4 (42).

Chemical Information

Molecular Formula C13H8N2OS
SMILEs O=c1nc(-c2ccccn2)sc2ccccc12
InChI InChI=1S/C13H8N2OS/c16-12-9-5-1-2-7-11(9)17-13(15-12)10-6-3-4-8-14-10/h1-8H
Molecular weight 240.04 Da
AlogP 2.7185000000000006
HBond acceptors 3
HBond donors --
Atoms 25

Vendors

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Expert Reviews

by SERP
(on 24 Sept 2020)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP
(on 18 Oct 2020)
Cellular Use Rating
In Model Organisms
This compound was discovered using a cellular assay in rat cardiomyocytes and characterized in rat H9c2 cells, so it is appropriate as a cellular probe in this context. Binding studies were done with...
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