For research use only. Not for therapeutic Use.
BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC50 between 6 and 100 nM)[1][2].
Since PD-1 mediated the exhaustion of natural killer (NK) cell by binding to its ligand PD-L1, BMS-1 (PD-1/PD-L1 inhibitor 1) (1 μM, 3 days) is used to disturb the interaction between PD-1 and PD-L1. Dexamethasone induced increase of PD-1 expression and decrease of cytotoxicity of the co-cultured NK92 cells are reversed by BMS-1[1]. BMS-1, a small-molecule immune checkpoint inhibitor of PD-1/PD-L1, can be used as a therapeutic strategy for tumor immunotherapy[2].
BMS-1 (500 μg/mL; 100 μL; i.p.) significantly increases the survival rates of the mVEGF165b group and mVEGF165b + MUC1 group[3].
Catalog Number | I013769 |
CAS Number | 1675201-83-8 |
Synonyms | (2S)-1-[[2,6-dimethoxy-4-[(2-methyl-3-phenylphenyl)methoxy]phenyl]methyl]piperidine-2-carboxylic acid |
Molecular Formula | C29H33NO5 |
Purity | ≥95% |
InChI | InChI=1S/C29H33NO5/c1-20-22(12-9-13-24(20)21-10-5-4-6-11-21)19-35-23-16-27(33-2)25(28(17-23)34-3)18-30-15-8-7-14-26(30)29(31)32/h4-6,9-13,16-17,26H,7-8,14-15,18-19H2,1-3H3,(H,31,32)/t26-/m0/s1 |
InChIKey | ZBOYJODMIAUJHH-SANMLTNESA-N |
SMILES | CC1=C(C=CC=C1C2=CC=CC=C2)COC3=CC(=C(C(=C3)OC)CN4CCCCC4C(=O)O)OC |
Reference | [1]. Zhao Y, et al. Depression Promotes Hepatocellular Carcinoma Progression through a Glucocorticoids Mediated Up-Regulation of PD-1 Expression in Tumor infiltrating NK Cells. Carcinogenesis. 2019 Feb 4. [2]. Li K, et al. Development of small-molecule immune checkpoint inhibitors of PD-1/PD-L1 as a new therapeutic strategy for tumour immunotherapy. J Drug Target. 2019 Mar;27(3):244-256. [3]. Zhang H, et al. Utilizing VEGF165b mutant as an effective immunization adjunct to augment antitumor immune response. Vaccine. 2019 Apr 3;37(15):2090-2098. [4]. Mengyuan Li, et al. KALRN mutations promote antitumor immunity and immunotherapy response in cancer. J Immunother Cancer. 2020 Oct;8(2):e000293. |