VISTA-IN-4

VISTA-IN-4 (Compound B3) is an orally active inhibitor of the immune checkpoint protein VISTA, with a KD of 0.452 ?M. It degrades VISTA in HepG2 cells with a degradation rate of 77% at a concentration of 5 ?M. VISTA-IN-4 counteracts VISTA-mediated immune suppression, restoring T cell activity and promoting the release of cytokine IL-2. Additionally, it exhibits antitumor activity in CT26 xenograft mouse models and demonstrates favorable pharmacokinetic properties, with good oral serum exposure in SD rats, reflected by an AUC (0-t) of 412.9 mg·h/mL.