Thermal stabilization of G-rich sequences of human and canine KIT promoter induced by 1 µM of candidate ligands (∆Tm °C) as well as of ligand concentrations (µM) causing a 50% displacement of TO (EC50)
| Compound | h_kit1 | d_kit1 | h_kit2 | d_kit2_A16 | dsDNA |
|---|---|---|---|---|---|
| AQ1 | |||||
| ∆Tm (°C) | 13.1 | 18.7 | 15.3 | ND | 4.6 |
| EC50 (µM) | 0.32 ± 0.05 | 0.64 ± 0.04 | 0.35 ± 0.05 | 0.14 ± 0.01 | 3.66 ± 0.08 |
| AN6 | |||||
| ∆Tm (°C) | 5.2 | 1.4 | 8.0 | 3.9 | 0.8 |
| EC50 (µM) | 4.11 ± 0.70 | 5.71 ± 0.46 | 3.63 ± 1.00 | 5.11 ± 0.29 | 11.42 ± 0.28 |
d_kit1, canine kit1 G4 forming sequence; d_kit2_A16, canine kit2 G4 forming sequence with the -159 G>A single nucleotide polymorphism; dsDNA, random double-strand DNA; h_kit1: human kit1 G4 forming sequence; h_kit2, human kit2 G4 forming sequence; ND, no detectable melting transition via thermal denaturation profiles; TO, thiazole orange.