PD-L1-IN-2

• CAT Number: I041188
• CAS Number: 2894733-91-4
• Molecular Formula: C33H38N4O6
• Molecular Weight: 586.68
• Purity: ≥95%
• Synonyms: tert-butyl N-[3-[[5-[(3,4-dimethoxyphenyl)methyl]-4-[(4-methoxyphenyl)methyl]-1-methylimidazol-2-yl]carbamoyl]phenyl]carbamate
• InChI: InChI=1S/C33H38N4O6/c1-33(2,3)43-32(39)34-24-10-8-9-23(20-24)30(38)36-31-35-26(17-21-11-14-25(40-5)15-12-21)27(37(31)4)18-22-13-16-28(41-6)29(19-22)42-7/h8-16,19-20H,17-18H2,1-7H3,(H,34,39)(H,35,36,38)
• InChIKey: WCBUHIGCYKSAAG-UHFFFAOYSA-N
• SMILES: CC(C)(C)OC(=O)NC1=CC=CC(=C1)C(=O)NC2=NC(=C(N2C)CC3=CC(=C(C=C3)OC)OC)CC4=CC=C(C=C4)OC

PD-L1-IN-2 is a potential tumor immunological agent by inhibiting PD-L1. PD-L1-IN-2 is a Naamidine J derivative and exerts antitumor effects in vivo by reducing PD-L1 expression and enhancing tumor-infiltrating T-cell immunity. PD-L1-IN-2 is used for colorectal cancer research[1].
PD-L1-IN-2 (compound 11c) is against RKO Cells with an IC50 value of 31.7μM[1].
PD-L1-IN-2 (0-10 μM; 0-24 hours) decreases PD-L1 expression in a dose-dependent and time dependent manner in RKO cells[1].
PD-L1-IN-2 (0-10 μM; 0-24 hours) promotes the turnover of PD-L1 protein.It shows the turnover rate of PD-L1 in PD-L1-IN-2-treated cells is faster than that in untreated cells in the CHX pulse-chase[1].
PD-L1-IN-2 (compound 11c) (i.p.; 25/50 mg/kg; once a day; 16 days) decreases the tumor sizes with an inhibition rate of 45% at 45 mg/kg, and the average tumor weight of the 50 mg/kg groups is significantly lower than that of the PBS group[1].

Reference

[1]. Pan-Pan Fu, et al. Bioactivity-Driven Synthesis of the Marine Natural Product Naamidine J and Its Derivatives as Potential Tumor Immunological Agents by Inhibiting Programmed Death-Ligand 1. J Med Chem. 2023 Apr 27;66(8):5427-5438.
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