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) |