BTZO-1

ARE Activator of MIF

Structure

Information

Protein target names: MIF

Mechanism of action: ARE Activator

Recommended in-cell concentration:
up to 1 uM

In Vitro Validations

Uniprot ID: P14174
Target Class: Other post-translational modification
Target SubClass: Tautomerase
Potency: Kd
Potency Value: 68.6 nM
Potency Assay: SPA binding assay with human protein
PDB ID for probe-target interaction (3D structure): 5B4O
Target aliases:
Macrophage migration inhibitory factor, MMIF, GLIF ...

DOI Reference: 10.1016/j.chembiol.2010.10.011

Uniprot ID: P14174
Target Class: Other post-translational modification
Target SubClass: Tautomerase
Potency: Kd
Potency Value: 147 nM
Potency Assay: SPA binding assay with rat protein
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Macrophage migration inhibitory factor, MMIF, GLIF ...

DOI Reference: 10.1016/j.chembiol.2010.10.011

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating

(last updated: 24 Sept 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

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 both rat and human proteins, establishing the Kd for each, but cellular effects in the original study were limited to rat. Importantly, this compound and its analogues did not substantially inhibit the tautomerase activity of its listed direct target, MIF, even at concentrations much higher than those required to observe substantial (presumably downstream) cellular effects, such as ARE activation and protection from induced apoptosis, suggesting that its ability to modulate the MIF interactome requires further investigation.

(last updated: 18 Oct 2020 )