SML2930

LH1307

≥97% (HPLC)

• Synonym(s): 2,2′-Dimethyl-3,3′-bis[2-methyl-4-(2-acetamidoethylamino)-methyl-5-(3-cyanopyridin-5-yl-methoxy)phenoxymethyl]-1,1′-biphenyl, LH 1307, LH-1307, N,N′-(2,2′-(4,4′-(2,2′-Dimethylbiphenyl-3,3′-diyl)bis(methylene)bis(oxy)bis(2-((5-cyanopyridin-3-yl)methoxy)-5-methyl-4,1-phenylene))bis(methylene)bis(azanediyl)bis(ethane-2,1-diyl))diacetamide
• Empirical Formula (Hill Notation): C₅₄H₅₈N₈O₆
• CAS Number: 2375720-38-8
• Molecular Weight: 915.09
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: powder
• storage condition: room temperature
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: N#CC1=CC(COC2=C(C=C(C(OCC3=C(C(C4=CC=CC(COC5=CC(OCC6=CN=CC(C#N)=C6)=C(C=C5C)CNCCNC(C)=O)=C4C)=CC=C3)C)=C2)C)CNCCNC(C)=O)=CN=C1

Description

Biochem/physiol Actions

LH1307 is a potent programmed cell death-1/programmed death-ligand 1 (PD-1 (CD279, PDCD1)/PD-L1 (B7-H1, PDCD1-L1)) protein-protein interaction (PPI) inhibitor (IC50 = 3 nM by HTRF assay) that induces symmetrically arranged PD-L1 homodimer formation by targeting PD-L1 at the PD-1 binding site. LH1307 effectively blocks cell surface PD-1/PD-L1 interaction between PD-1-expressing Jurkat cells and co-cultured PD-L1-expressing U2OS cells (SHP-1 recruitment IC50 = 79 nM) or co-cultured PD-L1-expressing aAPC/CHO-K1 cells (NFAT signaling restoration EC50 = 763 nM).

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable