FTO

Inhibitor

Inhibitor Characteristics

Mechanism of Action

Experimental Conditions

IC50 (µM)

Study

R-2-hydroxyglut-arate (R-2HG)

Competetive inhibitor

In vitro and in vivo for leukemia; in vitro for GBM

N/A but 300 used to show inhibition

Su et al. (2018), Qing et al. (2021)

Entacapone

Competetive inhibibitor

In silico;

in vitro for hepatocytes;

in vivo for metabolic study

3.5

Peng et al. (2019)

MA

Studied alone and in combination with an EGFR TKI (Gefitinib)

In vitro assay [92] [93] ;

in vitro for lung cancer;

clinical trials for GBM

4 - 12.5

Chen et al. (2022), Huang et al. (2015), Huff et al. (2021), Zeyen et al. (2022)

MA derivative: FB23-2

Direct inhibition, higher affinity than MA

In silico;

in vitro and in vivo for AML

2.6 ± 0.5

Huang et al. (2019)

MA derivative: MA2

Competetive inhibitor

In vitro and in vivo for

gastric cancer and GBM;

in vitro for HeLa cells

N/A but 20 - 120 used to show inhibition

Cui et al. (2017),

Shimura et al. (2022), Huang et al. (2015)

FTO-04

Selective competetive inhibitor

In silico;

in vitro for GBM

3.4

Huff et al. (2021)

Bisantrene (CS1) and Brequinar (CS2)

Tight, direct FTO inhibition

In silico;

in vitro and in vivo for AML and breast cancer;

bisantrene phase II clinical trials for AML;

in vitro for GBM

CS1: 0.02 - 0.8;

CS2: 0.06 - 10

Su et al. (2020),

Canaani et al. (2021)

Rhein

Inhibitor

In vitro assay;

in vivo for TNBC

30

Chen et al. (2012), Niu et al. (2019)

MO-I-500

Inhibitor

In vitro for TNBC

8.7

Singh et al. (2016)