PD-L1-IN-2 is a potential tumor immunological agent by inhibiting PD-L1. PD-L1-IN-2 is a Naamidine J derivative and exerts antitumor effects in vivo by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. PD-L1-IN-2 is used for colorectal cancer research.
PD-L1-IN-2 (compound 11c) is against RKO Cells with an IC50 value of 31.7μM[1]. PD-L1-IN-2 (0-10 μM; 0-24 hours) decreases PD-L1 expression in a dose-dependent and time dependent manner in RKO cells[1]. PD-L1-IN-2 (0-10 μM; 0-24 hours) promotes the turnover of PD-L1 protein.It shows the turnover rate of PD-L1 in PD-L1-IN-2-treated cells is faster than that in untreated cells in the CHX pulse-chase[1].
PD-L1-IN-2 (compound 11c) (i.p.; 25/50 mg/kg; once a day; 16 days) decreases the tumor sizes with an inhibition rate of 45% at 45 mg/kg, and the average tumor weight of the 50 mg/kg groups is significantly lower than that of the PBS group[1].
References:
[1]. Pan-Pan Fu, et al. Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1. J Med Chem. 2023 Apr 27;66(8):5427-5438.