VISTA inhibitor compound 1 is a bifunctional inhibitor targeting VISTA, shows good binding affinity with VISTA (SPR KD=256 nM), induces potent VISTA degradation in HepG2 cells and activates antitumor immunity.
VISTA inhibitor compound 1 (5 uM) significantly elevates the secretion of IFN-γ in PBMCs, activates antitumor immunity of PBMCs against MDA-MB 231 cells.
VISTA inhibitor compound 1 (10 uM) promotes autophagy-dependent degradation of VISTA through an autophagic pathway in HepG2 cells.
VISTA inhibitor compound 1 (30, 60, or 120 mg/kg) exhibits in vivo antitumor activity in a CT26 mouse model with no obvious body weight loss or mortality during the treatment.
VISTA inhibitor compound 1 significantly increases infiltration of CD8+ cells in tumor tissues in a dose-dependent manner, induces degradation of VISTA, shows better antitumor activity than CA-170 (Cat# PC-72654) at a dose of 60 mg/kg.