Table 2. Extended in Vitro Activity of Select Compounds.
| entry | compound | description | IC50 (nM) | CP50 (nM)a | stability (%)b | % cell deathc | % cell deathd |
|---|---|---|---|---|---|---|---|
| 1 | UNC10245092 | phage display peptide | 46 ± 13 | 3291 ± 397 | n.d. | 1.7 ± 2.0 | 9.5 ± 3.2 |
| 2 | UNC10245350 | TAT-UNC10245092 | 150 ± 40 | 2086 ± 423 | 0 | 57.1 ± 13.4 | 9.6 ± 8.8 |
| 3 | UNC10245351 | TAT-UNC10245092 neg | >10 000 | 2225 ± 124 | 0 | 1.1 ± 0.7 | 1.9 ± 1.3 |
| 4 | UNC10245131 | mRNA display hit 2 | 12 ± 7 | n.d. | 48.6 ± 21.4 | 2.7 ± 2.5 | 2.0 ± 2.2 |
| 5 | UNC10245234 | UNC10245131 K2A | 9 ± 3 | 440 ± 69 | 21.9 ± 19.0 | 2.7 ± 1.5 | 1.5 ± 1.3 |
| 6 | UNC10245496 | UNC10245131 analogue | 59 ± 16 | 438 ± 89 | 62.2 ± 8.3 | 3.4 ± 2.4 | 1.1 ± 0.4 |
a
CP50 measured using chloroalkane-tagged compounds
b
Stability as percent peptide remaining after 24 h in cell lysate.
c
MDA-MB-468 (CIB1-sensitive cell line) cell death.
d
MDA-MB-231 (CIB1-insensitive cell line) cell death.