Table 3.
Cdc25B Inhibitor Activity Profile
| SID | Cdc25B HTS % inhibition >50% | Cdc25B IC50 <50 μM | Selective vs. MKP-1/3 | Redox H2O2 generator | Cdc25B IC50 modulated | Inhibition of tumor cell proliferation |
|---|---|---|---|---|---|---|
| 850758 | + | + | − | + | + | NT |
| 845167 | + | + | − | + | + | NT |
| 4251194 | + | + | − | + | + | NT |
| 847359 | + | + | + | + | + | NT |
| 3712327 | + | + | + | + | + | NT |
| 845964 | + | + | − | + | + | NT |
| 7973677 | + | + | − | + | + | NT |
| 3712249 | + | + | − | + | + | NT |
| 856108 | + | + | + | + | + | NT |
| 8139964 | + | + | + | + | + | NT |
| 857882 | + | + | + | + | + | NT |
| 4242461 | + | + | − | + | + | NT |
| 4251929 | + | + | − | − | + | NT |
| 4249736 | + | + | − | − | + | NT |
| 4249621 | + | + | − | − | − | NT |
| 4241893 | + | + | − | − | − | NT |
| 844096 | + | + | − | − | − | NT |
| 850390 | + | + | + | − | − | − |
| 843791 | + | + | + | − | − | − |
| 7964733 | + | + | − | − | + | NT |
| 851514 | + | + | + | − | − | − |
| 847214 | + | + | + | − | − | − |
| 4260465 | + | + | + | − | − | + |
| 4258795 | + | + | + | − | − | + |
| 4248661 | + | + | + | − | + | NT |
Cdc25B HTS % inhibition >50%, inhibition >50% in the primary Cdc25B screen; Selective vs. MKP-1/3, selectivity for Cdc25B versus MKP-1 and/or MKP-3; Redox H2O2 generator, evidence of redox cycling H2O2 generation; Cdc25B IC50 modulated, the inhibition of Cdc25B was sensitive to the modifications in the assay conditions described in Table 1; Inhibition of tumor cell proliferation, the ability to inhibit the proliferation of the human MBA-MD-435 breast and PC-3 prostate cancer cell lines. NT = not tested. + indicates that the compound met this criterion; – indicates that the compound did not meet this criterion.