Table 1.
ΔTm in 60 mM K+ at 1 µM compound in the FRET-melting assays.
| Ligand | duplex[a] | H-Telo | c-kit1 | c-kit2 | c-myc | bcl2 | k-ras |
|---|---|---|---|---|---|---|---|
| ΔTm max in °C[b] |
32.8 ±1.2 |
36.1 ±1.3 |
41.0 ±1.5 |
22.8 ±0.7 |
16.2 ±1.1 |
32.1 ±0.9 |
49.6 ±1.4 |
| 1 | 0.7 | 24.0 | 16.0 | 21.4 | 6.2 | 14.6 | 7.3 |
| 2 | 0.0 | 3.6 | 10.1 | 4.4 | 2.1 | 0.5 | 2.8 |
| 3 | 1.1 | 22.4 | 15.1 | 17.6 | 14.3 | 18.9 | 20.8 |
| 4 | 3.9 | 36.5 | 39.1 | 21.5 | 17.0 | 30.7 | 48.4 |
| 5 | 0.0 | 0.5 | 2.7 | 0.0 | 0.2 | 0.0 | 0.0 |
| 6 | 1.6 | 29.0 | 13.4 | 4.8 | 16.4 | 13.4 | 10.5 |
| 7 | 1.3 | 36.4 | 37.9 | 16.8 | 16.4 | 30.8 | 24.1 |
| 8 | 0.0 | 35.1 | 24.0 | 15.9 | 17.0 | 19.9 | 14.2 |
| 9 | 0.6 | 22.1 | 20.2 | 9.9 | 8.5 | 12.3 | 18.4 |
| 10 | 3.1 | 34.8 | 25.8 | 21.0 | 16.5 | 27.7 | 26.8 |
| 11 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.2 |
| 12 | 0.0 | 2.8 | 6.1 | 2.8 | 1.4 | 0.2 | 1.8 |
[a]
Duplex formed by two complementary strands linked via hexaethyleneglycol (HEG) loop.
[b]
This value corresponds to 95.5°C - Tm (in °) for quadruplex alone as 95.5°C is the maximal temperature measurable in this assay.