SML2930

LH1307

≥97% (HPLC)

• Synonym(e): 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
• Empirische Formel (Hill-System): C₅₄H₅₈N₈O₆
• CAS-Nummer: 2375720-38-8
• Molekulargewicht: 915.09
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥97% (HPLC)
• Form: powder
• Lagerbedingungen: room temperature
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 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
• InChI: 1S/C54H58N8O6/c1-35-17-47(29-57-13-15-61-39(5)63)53(65-31-43-19-41(23-55)25-59-27-43)21-51(35)67-33-45-9-7-11-49(37(45)3)50-12-8-10-46(38(50)4)34-68-52-22-54(66-32-44-20-42(24-56)26-60-28-44)48(18-36(52)2)30-58-14-16-62-40(6)64/h7-12,17-22,25-28,57-58H,13

Beschreibung

Biochem./physiol. Wirkung

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).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable