BTZO-1

ARE Activator of MIF

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(1 ratings)

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Probe BTZO-1 is in the process of SERP review.

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Information

ARE Activator

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

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

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 24 Sept 2020 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP 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 )