Table 3.
Candidate compounds targeting m6A regulators for cancer therapy.
| Target | Compound | IC50 (μm) | Functions |
|---|---|---|---|
| METTL3 | Adenosine 2 | 8.7 | METTL3 inhibitor [302] |
| METTL3 | UZH1a | 7 | METTL3 inhibitor, reduces the m6A/A ratio in mRNAs of three AML cell lines [303] |
| METTL3 | STM2457 | 0.0169 | METTL3 inhibitor, reduces AML growth and increases differentiation and apoptosis [294] |
| FTO | Rhein | 21 | FTO inhibitor, exhibits good inhibitory activity on m6A demethylation inside cells [288] |
| FTO | MO‐I‐500 | 8.7 | FTO inhibitor, shows anti‐convulsant activity [304] |
| FTO | Meclofenamic acid | 8 | FTO inhibitor [289] |
| FTO | CHTB | 39.24 | FTO inhibitor [305] |
| FTO | R‐2HG | 133.3 | FTO inhibitor, exerts a broad anti‐leukemic activity in vitro and in vivo [166] |
| FTO | FB23‐2 | 2.6 | FTO inhibitor, suppresses proliferation and promotes the differentiation/apoptosis of human AML cell lines [292] |
| FTO | Entacapone | 3.5 | FTO inhibitor, mediates metabolic regulation through FOXO1 [291] |
| FTO | CS1 | 0.14 | FTO inhibitor, suppresses cancer stem cell maintenance and immune evasion [306] |
| FTO | CS2 | 2.6 | FTO inhibitor, suppresses cancer stem cell maintenance and immune evasion [306] |
| FTO | Saikosaponin‐d | 0.46 | FTO inhibitor, shows a broadly suppressed AML cell proliferation and promoted apoptosis and cell‐cycle arrest both in vitro and in vivo [307] |
| FTO | Dac51 | 0.4 | FTO inhibitor, blocks FTO‐mediated immune evasion, and synergizes with checkpoint blockade for better tumor control [308] |
| FTO | FTO‐4 | 3.4 | FTO inhibitor, prevents neurosphere formation in patient‐derived GBM stem cells [309] |
| FTO | 18097 | 0.64 | FTO inhibitor, shows anti‐cancer activities both in vitro and in vivo [310] |
| ALKBH5 | MV1035 | / | ALKBH5 inhibitor, shows an inhibitory effect on GBM [311] |
| ALKBH5 | ALK‐04 | / | ALKBH5 inhibitor, enhances the efficacy of cancer immunotherapy [244] |
| ALKBH5 | 2‐[(1‐hydroxy‐2‐oxo‐2‐phenylethyl)sulfanyl]acetic acid | 0.84 | ALKBH5 inhibitor, suppresses cell proliferation at low micromolar concentrations in AML [312] |
| ALKBH5 | 4‐[(furan‐2‐yl)methyl]amino‐1,2‐diazinane‐3,6‐dione | 1.79 | ALKBH5 inhibitor, suppresses cell proliferation at low micromolar concentrations in AML [312] |
| ALKBH5 | Compound 20m | 0.021 | ALKBH5 inhibitor [313] |
| IGF2BP1 | BTYNB | 5 | IGF2BP1 inhibitor, targes c‐Myc and inhibits melanoma and ovarian cancer cell proliferation [314] |
| IGF2BP1 | 7773 | 30.45 | IGF2BP1 inhibitor, represses Kras and a pro‐oncogenic phenotype in LUAD [315] |
| IGF2BP2 | Benzamidobenzoic acid class and ureidothiophene clas | / | IGF2BP2 inhibitors, show anti‐cancer activities both in vitro and in vivo [316] |