生物活性

• 靶点	PD-1/PD-L1 IC50:18nM

• 描述Activation of PD-1/PD-L1 signaling can induce T-cell hybridoma apoptosis, as well as negatively regulate antigen-specific T-cell-mediated immunologic responses. Also, PD-1/PD-L1 signaling blockade is an effective cancer immunotherapy. PD-1/PD-L1 inhibitor 2 (also called BMS202) is a small-molecule PD-1/PD-L1 interaction inhibitor with IC50 value of 18nM. Blockade of the PD-1 /PD-L1 ligation can enhance the immune response and improve T cell activity in chronic infection systems, as well as enhance the responses to therapeutic vaccination. Within concentrations ranging in 0.01-10μΜ, PD1-PDL1 Inhibitor 2 could improve the immune response to a tumor antigen, a viral antigen, a bacterial antigen or any pathogen in a subject by provoking and amplifying autoimmune responses. Incubation with PD1-PDL1 Inhibitor 2 could stabilize PD-L1 thermally and induce unfolding of PD-L1, while PD-L2 was characterized by a comparable melting temperature. In a crystal structure of PD1-PDL1 Inhibitor 2/PD-L1 complex, PD1-PDL1 Inhibitor 2 binds at a hydrophobic cavity forming upon PD-L1 dimerization. PD1-PDL1 Inhibitor 2 dissociated PD-1/PD-L1 interaction at stoichiometric concentration, consistent with the estimated KD of the PD-1/PD-L1 complex of 8μM, which is specific for PD-L1.