Table 1.

Inhibitory effects of PEP005 in a panel of characterized cell lines

Cell lineMain characteristics*
PEP005 IC50 ± SD (μmol/L)
p53PKCαPKCδ1 h24 h48 h
Colon
    HT29mutLowHigh240 ± 28110 ± 35140 ± 28
    HCT116wtLowLow>400>400120 ± 24
    Colo205mutHighInt20 ± 723 ± 80.01 ± 0.002
    HCC2998mutLowHigh31 ± 940 ± 1430 ± 6
Breast
    MCF7wtLowLow290 ± 60210 ± 36180 ± 36
    MDA-MB-435mutLowHigh90 ± 2395 ± 302.6 ± 0.52
Ovarian
    OVCAR3mutHighLow350 ± 85270 ± 50200 ± 40
    IGROV1wtLowLow250 ± 65270 ± 62200 ± 42
Lung
    Hop62mutHighLow200 ± 46110 ± 35110 ± 22
    Hop92mutHighHigh230 ± 78210 ± 5285 ± 17
  • Abbreviations: wt, wild-type; mut, mutated; Int, intermediate expression in relation to average for 60 cancer cell lines.

  • * National Cancer Institute screen.