Drug intelligence / Profile preview

Dac51

Development stage
Preclinical
Modality
Small Molecules
Administration
None
01

Overview

Dac51 is a potent, cell-active small molecule inhibitor of the RNA demethylase FTO (Fat mass and obesity-associated protein). Dac51 inhibits FTO-mediated N6-methyladenosine (m6A) RNA demethylation with an IC50 of 0.4 µM, leading to increased m6A abundance on target transcripts. In preclinical models, Dac51 downregulates bZIP family transcription factors, alters glycolysis-related genes, and demonstrates antitumor activity by enhancing T cell infiltration and synergizing with immune checkpoint blockade agents. It was developed through optimization of the prior FTO inhibitor FB23 and is used primarily as a research compound in oncology models. Dac51 is not approved for human therapeutic use.[1][4][6]

02

Targets

FTO (Fat mass and obesity-associated protein)

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