ISQ-1 is a potent in vitro inhibitor of several cancer cell lines (LS174T cell proliferation, IC50=100 nM), inhibits Wnt signaling and also activates adenosine monophosphate kinase (AMPK).
ISQ-1 inhibits in vitro cell growth of colon cancer LS174T, prostate cancer PC-3, sarcoma SK-LMS-1 and liver cancer HepG2 cell lines at nanomolar concentrations.
ISQ-1 also inhibits Wnt signaling target genes including c-Myc and axin2 and activates AMPK in a dose-dependent manner.
ISQ-1 inhibits mitochondrial ETC (electron transport chain) complex I in LS174T cells.
ISQ-1 synergizes with PLK inhibitor BI2536, inhibits the G2/M transition on cell cycle of LS174T colorectal cancer cells.
ISQ-1 (100 nM, 300 nM) inhibits mouse colon cancer organoids from Apcf/+/KrasLSL-G12D/Villin-Cre mouse model.
ISQ-1 (20 mg/kg/day) and the Plk1 inhibitor BI2536 (30 mg/kg twice a week) synergistically induced regression of LS174T colon cancer cell xenografts in nude mice.