Table 1. Structure-Activity Relationship of Skp2-Cks1 Inhibitors.
Compound | Structure | Inhibition of Skp2-Cks1 IC50 (μM) | p27 Ub IC50 (μM) |
---|---|---|---|
857 | 36 ± 6.2 | ~30 | |
Q857 | 71 ± 4.4 | ~15 | |
A857 | 1090 ± 189 | >300 | |
E857 | 8311 ± 1458 | >300 | |
MHQ | 434 ± 39.5 | >300 | |
BQ | 626 ± 65.7 | >300 | |
NSC681152 | 75.6 ± 6.8 | ~80 |
BQ, 1,4-benzoquinone; MHQ, methylhydroquinone.