Table 1. Activity of fascaplysin, BPT and other structural analogues in different in vitro kinase assays and DNA-binding (EtBr displacement) assay.
| In vitro bioassay |
IC50 (mean±S.D.) (μM) |
||||
|---|---|---|---|---|---|
| CA198 (3) | CA199 (4) | CA211 (5) | BPT (6) | Fascaplysin (1) | |
| Cdk4-cyclin D1 | 25±5.5 | 24.4±4 | 44±3 | 10±1.2 | 0.41±0.04 |
| Cdk2-cyclin A | 861±29 | 766±33 | 720±24 | 831±15.5 | >250 |
| Cdk1-cyclin B1 | >500 | >500 | >500 | >500 | >250 |
| Cdk9-cyclin T1 | >1000 | >1000 | >1000 | >1000 | >250 |
| Cdk5-p35 | ND | ND | ND | NI | ND |
| Cdk6-cyclin D1 | ND | ND | ND | NI | ND |
| Cdk7-cyclin H | ND | ND | ND | NI | ND |
| EGFR | ND | ND | ND | NI | ND |
| GSK3β | ND | ND | ND | NI | ND |
| MAPK1 | ND | ND | ND | NI | ND |
| MEK1 | ND | ND | ND | NI | ND |
| PDGFR | ND | ND | ND | NI | ND |
| Plk3 | ND | ND | ND | NI | ND |
| PKA | ND | ND | ND | NI | ND |
| PKCα | ND | ND | ND | NI | ND |
| IGF-1 R | ND | ND | ND | NI | ND |
| EtBr displacement assay | No EtBr displacement up to 100 μM | No EtBr displacement up to 100 μM | No EtBr displacement up to 100 μM | No EtBr displacement up to 100 μMa | Displaces EtBr at 1 μM |
Abbreviations: ND, not determined; NI, no inhibition up to 10 μM
IC50 values are presented in μM concentration. The IC50 values presented here are means and S.D. from three independent experiments
a
Detailed results of DNA-binding studies are provided in Section S5 of the Supplementary Information