PD-1/PD-L1 Inhibitor

PD-1/PD-L1-IN-58 (compound 2) is a novel inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-58 selectively binds to PD-L1 over PD-1, with a dissociation rate constant (K_D) value of 77.60  nM. PD-1/PD-L1-IN-58 has oral activity. PD-1/PD-L1-IN-58 can be used in the research of influenza A virus.

BMS-1166 (Standard) is the analytical standard of BMS-1166 (HY-102011). This product is intended for research and analytical applications. BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC₅₀ of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.

CA-170 (Standard) is the analytical standard of CA-170 (HY-101093). This product is intended for research and analytical applications. CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes.

LH1306 is a C2-symmetric inhibitor of PD-₁/PD-L₁ protein-protein interaction (PPI), with an IC₅₀ value of 25 nM. LH1306 can be used in anti-tumor research.

Cilengitide hydrochloride (EMD 121974 hydrochloride) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide hydrochloride inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide hydrochloride inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide hydrochloride can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

PD-L1/LpxC-IN-1 (Conpound 12b) is the inhibitor for PD-L1 and LpxC with IC₅₀ of 5.2 μM and 0.081 μM. PD-L1/LpxC-IN-1 inhibits the biosynthesis of bacterial lipopolysaccharide, causes the lysis and death of bacterial cells. PD-L1/LpxC-IN-1 inhibits Gram-negative bacteria, MIC for K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028 and P. aeruginosa ATCC 9027 is 0.25-0.5 μg/mL. PD-L1/LpxC-IN-1 downregulates the expression of inflammatory factors IL-2 and IFN-γ, upregulates the expression of CD4+ and CD8+ cells, thereby activating the immune system and inhibiting excessive inflammatory responses. PD-L1/LpxC-IN-1 exhibits antibacterial activity in K. pneumoniae ATCC 13883 infected mouse models.

CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC₅₀ of 0.36 μM. CSN5-IN-2 can increase the level of Cullin 1 neddylation, and downregulate the expression of RAD51 and PD-L1 in cancer cells. CSN5-IN-2 has anti-tumor activity, and its effect is better when combined with Talazoparib (HY-16106).

Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) is rat-derived IgG2b κ type antibody inhibitor, targeting to PD-L1/B7-H1. Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) can block PD-L1/ B7-1 interactions and does not block PD-L1/PD-1 interactions. Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) can be used for the researches of cancer, infection, immunology and metabolic disease, such as MB49 tumor, heart graft and diabetes.

Ertabresib (Standard) (INCB-057643 (Standard)) is the analytical standard of Ertabresib (HY-111485). This product is intended for research and analytical applications. Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer.