Table 2.
Inhibitory and translation properties of dinucleotide cap analogues modified at N2 position of 7-methylguanosine
| Compound | IC50 [µM] | Translational properties of mRNA capped | |||
|---|---|---|---|---|---|
| Ascaris suum | Rabbit reticulocyte lysate (RRL) | RRL | HEK293 cells | ||
| Relative translation efficiency | Relative cap-dependent translation efficiency | Relative total protein expression | |||
| m7GMP | >50 | >50 | − | − | − |
| m7GTP | 6.1 | 2.3 ± 0.20 | − | − | − |
| m7GpppG | − | 8.94 ± 0.86 | 1 | 1 | 1 |
| ARCA | − | − | 1.56 ± 0.03 | 1.65 ± 0.06 | 1.46 ± 0.50 |
| 22 | − | 1.7 ± 0.16 | 1.72 ± 0.28 | 1.82 ± 0.34 | 2.87 ± 0.50 |
| 23 | − | 4.46 ± 0.53 | 1.39 ± 0.19 | 1.44 ± 0.22 | 3.30 ± 0.86 |
| 24 | − | 4.12 ± 0.35 | 1.29 ± 0.17 | 1.35 ± 0.20 | 2.42 ± 0.30 |
| 25 | − | 0.61 ± 0,04 | 3.30 ± 0.77 | 3.52 ± 0.82 | 1.80 ± 0.34 |
| 26 | − | 0.89 ± 0,12 | 2.76 ± 0.54 | 2.94 ± 0.53 | 2.18 ± 0.91 |
| 27 | − | 0.98 ± 0,13 | 3.29 ± 0.74 | 3.52 ± 0.73 | 2.29 ± 0.12 |
| 28 | − | 1.30 ± 0,23 | 2.65 ± 0.89 | 2.80 ± 0.90 | 1.96 ± 0.05 |
| 29 | − | 0.57 ± 0,06 | 3.37 ± 0.84 | 3.51 ± 0.82 | 1.64 ± 0.09 |
| 30 | − | 1.87 ± 0,08 | 1.92 ± 0.43 | 2.00 ± 0.44 | 1.42 ± 0.20 |