Table 1 Activity of fascaplysin, BPT and other structural analogues in different in vitro kinase assays and DNA-binding (EtBr displacement) assay
From: Antitumour potential of BPT: a dual inhibitor of cdk4 and tubulin polymerization
In vitro bioassay | IC 50 (mean±S.D.) ( μ M) | ||||
|---|---|---|---|---|---|
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 |
