VPC-18005 is a luciferase inhibitor. VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain thereby disrupting the ERG binding to DNA.
VPC-18005 (1 and 10 µM) produced a 20–30% decrease in the dissemination of cancer cells in zebrafsh. VPC-18005 (5 µM) inhibits pETS-luc reporter activity with IC50s of 3 and 6 μM in PNT1B-ERG and VCaP cells, respectively. VPC-18005 antagonizes the metastatic potential of ERG-expressing prostate cells and suppresses ERG reporter activity without exhibiting overt cytotoxicity. VPC-18005 inhibits migration and invasion of ERG-overexpressing cells in vitro.