VT02956 is a potent, specific inhibitor of Hippo pathway kinase LATS with IC50 of 0.76 nM (LATS1) and 0.52 nM (LATS2), respectively;
VT02956 reduces YAP/TAZ phosphorylation in both dose- and time-dependent manner with IC50 of 0.16 μM and 0.43 μM in HEK293A cells and 4T1 cells, respectively.
VT02956 suppresses ESR1 transcription, dramaticly reduces ERα and its target genes TFF1 and GREB1.
VT02956 targets the LATS-YAP/TAZ-ERα axis to inhibit ER+ tumours cell growth, inhibits the proliferation of MCF-7 and T47D cells.
VT02956 inhibits the growth of T47D cells with hormone therapy resistant ESR1 mutation (ERa Y537S or D538G), enhances the anti-tumour effect of palbociclib in ER+ breast cancer cells.
