YUM70 (YUM-70) is a derivative of 8-hydroxyquinoline targeting GRP78, and cytotoxic to pancreatic cancer cell lines (MIA PaCa-2 cell IC50=2.5 uM).
YUM70 dose-dependently decreased PANC-1 and UM59 cell proliferation in 3D-culture systems (IC50<10 uM).
YUM70 upregulates UPR target proteins and induces ER stress and apoptosis via phosphorylation of eIF2α.
YUM70 binds to full-length GRP78 and causes a positive shift in the melting temperature (Tm) of GRP78 in a dose-dependent manner.
YUM70 inhibits GRP78 ATPase activity of the full-length protein with IC50 of 1.5 uM.
YUM70 can up-regulate GRP78 transcription and protein levels.
YUM70 reduces tumor growth in a MIA PaCa-2 xenograft model.
