QP73

QP73 : Degrader (PROTAC) of FTO

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe QP73 is in the process of SERP review.

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Information

Degrader (PROTAC)

up to 1 uM

In Vitro Validations

Uniprot ID: Q9C0B1

Target Class: Enzyme

Target SubClass: FTO family

Potency: IC50

Potency Value: 1790 nM

Potency Assay: Inhibition of FTO demethylation via cell-free dot blot assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Alpha-ketoglutarate-dependent dioxygenase FTO, KIA ...

DOI Reference: 10.1016/j.apsb.2024.07.016

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): Quantitative proteomic analysis was performed on NB4 cells treated with 300 nM QP73 and found FTO was depleted after 36 h.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Relevant signaling pathways are identified but off-target effects of the FTO PROTAC degrader QP73 on other m6A modifying proteins and broader profiling outside target family are lacking. A recent paper challenges the current understanding of FB23-2 (a fluorine analog of Dac85) as a selective FTO inhibitor, demonstrating it’s primary action on hDHODH (ACS Pharmacol. Transl. Sci. 2024, 7, 12, 4096–4111). As the selectivity/off-target profile remains underexplored, the compound should be used with caution.

(last updated: 13 Feb 2025 )