BMSpep-57 hydrochloride 是一种有效的大环肽类抑制剂，抑制 PD-1/PD-L1 相互作用，IC50 为 7.68 nM。BMSpep-57 hydrochloride 与 PD-L1 结合，MST 和 SPR 测定表明，Kd 分别为 19 nM 和 19.88 nM。BMSpep-57 hydrochloride 通过增加 PBMC 中 IL-2 的产生促进 T 细胞功能。
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs[1].
In a ELISA competition assay, BMSpep-57 inhibits PD-1/PD-L1 binding up to 98.1% 300 nM. And it shows a concentration dependent inhibition of PD-1/PD-L1 binding with an IC50 of 7.68 nM[1].BMSpep-57 induced high levels of IL-2 at 1 µM and 500 nM concentrations in SEB-stimulated peripheral blood mononuclear cells[1].BMSpep-57 (0.2-10 μM; 24 hours) does not show any effect on the Jurkat, CHO and HepG2 cells’ viability at the various concentrations tested[1].
[1]. Aravindhan Ganesan, et al. Comprehensive in vitro characterization of PD-L1 small molecule inhibitors.Sci Rep . 2019 Aug 27;9(1):12392.
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