PD-L1-IN-12

PD-L1-IN-2 (compound SA13) (recombinant Tag1-PD-L1 and Tag2-PD-1 proteins; 3 h) strongly inhibited the PD-1/PD-L1 interaction with IC₅₀ = 5.2 nM^[1].
PD-L1-IN-2 (recombinant hPD-L1 Protein (HY-P73361); 15-960 nM) exhibits a strong binding affinity to the hPD-L1 protein with K_D = 9.06 nM^[1].
PD-L1-IN-2 (1-32 μM; 48 h) exhibits minimal direct cytotoxicity across various tumor cell lines (hPD-L1MC38, MDA-MB-231, RKO, SK-N-SH, NCI-H292, SK-N-AS, MCF-7, HT-29, A549) and normal cells (MRC-5, PBMCs), showing non-specific cytotoxicity only at very high concentrations^[1].
PD-L1-IN-2 (100 nM or 7.8-1000 nM; 30 min) effectively blocks the binding between PD-1 and PD-L1 proteins in HEK-293T cells (co-incubated with exogenous PD-L1-Fc protein) with IC₅₀ = 25.26 nM^[1].
PD-L1-IN-2 (1 μM or 0.008-8 μM; 16 h) downregulates cell-surface PD-L1 expression in a significant, dose-dependent manner and induces PD-L1 internalization in tumor cells (hPD-L1MC38 (IC₅₀ = 113.6 nM)、MDA-MB-231 (IC₅₀ = 378.5 nM)、RKO (IC₅₀ = 101.0 nM))^[1].
PD-L1-IN-2 (0.016-8 μM; 16 h) also significantly induces the downregulation of cell-surface PD-L1 expression in HEK-293T cells overexpressing PD-L1-GFP (IC₅₀ = 517.1 nM), confirming that this downregulation results from internalization rather than epitope competition or steric masking^[1].
PD-L1-IN-2 (1-8 μM) does not reduce total PD-L1 protein expression in hPD-L1MC38 cells^[1].
PD-L1-IN-2 (1 μM; 8 h) significantly induces the co-localization of internalized PD-L1 with the early endosome marker Rab5 in HEK-293T cells overexpressing PD-L1-GFP^[1].
PD-L1-IN-2 (1-8 μM; 48 h) reverses the immunosuppressive effects of PD-L1 in a dose-dependent manner in CD3/CD28 antibody-activated PBMCs (co-incubated with exogenous PD-L1 protein), effectively restoring the ability of suppressed T cells to secrete interferon-gamma (IFN-γ)^[1].
PD-L1-IN-2 (1-32 μM; 48 h) induces significant, dose-dependent immune-mediated cytotoxicity against tumor cells with high PD-L1 expression (hPD-L1MC38, MDA-MB-231), while exhibiting no significant cytotoxicity against tumor cell lines with low PD-L1 expression (MCF-7, A549) n a co-culture system of tumor cells and PBMCs (tumor cell:PBMC ratio of 1:10). PD-L1-IN-2 promotes PBMC-mediated immune killing of tumor cells primarily by blocking the PD-1/PD-L1 axis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.