Table 1.
Selectivity summary for VLS-1272 against a panel of human and mouse kinesins
| Kinesin | ATP (mM) | IC50 (nM), 30–60 min | IC50 (nM), 24 h |
|---|---|---|---|
| Human KIF18A | 0.10 (1 x KM) | 41 ×/ ÷ 1.1 (n = 3) | |
| 1.0 (10 x KM) | 9.3 ×/ ÷ 1.4 (n = 11) | 0.58 ×/ ÷ 1.4 (n = 13) | |
| Murine KIF18A | 0.10 (1 x KM) | 8.8 ×/ ÷ 1.2 (n = 3) | |
| Human KIF19 | 0.030 (1.5 x KM) | 280 (n = 2) | 150 (n = 1) |
| Human KIF18B | 0.030 (1.5 x KM) | >100,000 (n = 1) | |
| Human KIF11/Eg5 | 0.030 (6 x KM) | >100,000 (n = 1) | |
| Human KIFC1 | 0.010 (1 x KM) | >100,000 (n = 1) |
Inhibitory activity of VLS-1272 against the proteins listed using ADP-Glo assay to measure ATPase activity.