PD-L1-IN-3 (Compound 4a) is a compound that targets PD-1/PD-L1, the IC50 value and EC50 value is 4.97nM and 2.70 μM for inhibit PD-L1 and Jurkat T cells, respectively. PD-L1-IN-3 can bind PD-L1 dimer to prevent PD-1 binding to PD-L1, therefore blocking PD-1 signaling. PD-L1-IN-3 can be used for lung cancer and melanoma diseases research.
PD-L1-IN-3 (Compound 4a) (0.01-100 μM, 40 min) disrupts the binding between PD-1 and PD-L1 and enhances a TCR-mediated activation of the Jurkat cells[1].PD-L1-IN-3 (0.01-100 μM, 40 min) has higher uptake which correlated with PD-L1 expression in PD-L1+ H358 tumors[1].
References:
[1]. Ważyńska MA, et al. Design, Synthesis, and Biological Evaluation of 2-droxy-4-phenylthiophene-3-carbonitrile as PD-L1 Antagonist and Its Comparison to Available Small Molecular PD-L1 Inhibitors. J Med Chem. 2023 Jul 27;66(14):9577-9591.