Thermal denaturation studies (Tm values) of different ODN with complementary RNA and their degradation against mouse liver homogenates137.
ODN (5′ → 3′)a | T m with RNA (°C) | Mouse liver homogenatesb | RNase-H activityc | IC50 (nM) |
---|---|---|---|---|
d(GLMeCLATTGGTATTLMeCLAL) | 59.4 | —d | 5.8 | 93 |
d(GLMeCLA3′SPTTGGTATTLMeCLAL) | 60.0 | 68 | 17.3 | 8833 |
d(GLMeCLA5′SPTTGGTATTLMeCLAL) | 58.5 | 56 | 9.9 | 410 |
d(GLMeCLAT3′SPTGGTATTLMeCLAL) | 62.5 | 34 | 13.6 | 936 |
d(GLMeCLAT5′SPTGGTATTLMeCLAL) | 57.4 | 56 | 11.4 | 340 |
d(GLMeCLATTGG3′SPTATTLMeCLAL) | 62.5 | 1.2 | 10.0 | 1345 |
d(GLMeCLATTGG5′SPTATTLMeCLAL) | 58.5 | 41 | 11.3 | —d |
d(GLMeCLATTGGTA3′SPTTLMeCLAL) | 61.9 | 1.5 | 9.8 | 1129 |
d(GLMeCLATTGGTA5′SPTTLMeCLAL) | 59.0 | 31 | 56.9 | —d |
3′SP and 5′SP refer to the 3′-SP and the 5′-SP linkages respectively. L refers to LNA residues.
% intact gapmer at the end of the experiment.
% full length target RNA after 48 h of incubation.
Gapmer ODN not tested.