2. Signaling Pathways
  3. Immunology/Inflammation
  4. PD-1/PD-L1

PD-1/PD-L1

PD-1/Programmed death-ligand 1

PD-1/PD-L1

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Programmed death-1 (PD-1) is a cell surface receptor that functions as a T cell checkpoint and plays a central role in regulating T cell exhaustion. PD-1 is activated by the engagement of its ligands PDL-1 or PDL-2. PD-1 receptor delivers inhibitory checkpoint signals to activated T cells upon binding to its ligands PD-L1 and PD-L2 expressed on antigen-presenting cells and cancer cells, resulting in suppression of T-cell effector function and tumor immune evasion. Inhibiting the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) pathway is an attractive strategy for tumor immunotherapy.

PD-1 is expressed on activated T cells, B cells, monocytes, dendritic cells (DCs), regulatory T cells (Tregs), and natural killer T cells (NKT). It is a member of a family of immunoglobulin domain (Ig) co-receptors that modify the outcome of activation of the T cell receptor by an antigen-presenting cell (APC) or infected target cell. PD-L1 is widely and constitutively expressed on both hematopoietic and nonhematopoietic cells; e.g., naive T and B cells, vascular endothelial cells, and pancreatic islet cells, whereas PD-L2 is exclusively and inducibly expressed on professional APCs.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-171331
    AB-3PRGD2
    		Inducer
    AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.
    AB-3PRGD2
  • HY-160585
    PD-L1/PD-1-IN-1
    		Inhibitor
    PD-L1/PD-1-IN-1 (compound 8j) is a potent inhibitor of PD-L1/PD interaction, with IC50 ＜ 1 nM. PD-L1/PD-1-IN-1 plays an important role in anti-tumor research.
    PD-L1/PD-1-IN-1
  • HY-P10950
    PD-L1 inhibitory peptide
    		Inhibitor
    PD-L1 inhibitory peptide is an inhibitor peptide targeting programmed cell death ligand 1 (PD-L1). PD-L1 inhibitory peptide binds to PD-L1, relieving immunosuppression and restoring the antitumor activity of T cells. PD-L1 inhibitory peptide is promising for research of cancers.
    PD-L1 inhibitory peptide
  • HY-172133
    HDAC3-IN-6
    		Activator
    HDAC3-IN-6 (Compound SC26) is a selective HDAC3 inhibitor with an IC50 of 53 nM. HDAC3-IN-6 dose-dependently induces the expression of PD-L1. HDAC3-IN-6 induces more pronounced Apoptosis and production of ROS. HDAC3-IN-6 exhibits high antitumor efficacy against colorectal cancer.
    HDAC3-IN-6
  • HY-P990014
    Danburstotug
    		Inhibitor
    Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) human monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic.
    Danburstotug
  • HY-156202
    Geranylgeranoic acid
    		Inhibitor
    Geranylgeranoic acid (Compound 5) is inhibits lysine-specific demethylase 1 (LSD1) with an IC50 value of 46.97 µM. Geranylgeranoic acid induces apoptosis via loss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32) in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes. Geranylgeranoic acid an isoprenoid with anticancer activity, which is found in S. chinensis.
    Geranylgeranoic acid
  • HY-P3139A
    TPP-1 TFA
    		Inhibitor
    TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function.
    TPP-1 TFA
  • HY-P991353
    Sym-021
    		Antagonist
    Sym-021 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. Sym-021 blocks the binding of PD-L1 and PD-L2 ligands, inducing the secretion of interferon IFN-γ and IL-2 and the proliferation of T cells. Sym-021 has anti-tumor activity in PDX mouse models.
    Sym-021
  • HY-145770
    PD-1/PD-L1-IN-19
    		Inhibitor
    PD-1/PD-L1-IN-19 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-19 blocks PD-1/PD-L1 with the IC50 of 62.3 nM. PD-1/PD-L1-IN-19 can be used for the research of cancers, infectious diseases and autoimmune diseases.
    PD-1/PD-L1-IN-19
  • HY-162614
    Rogersonin E
    		Inhibitor
    Rogersonin E can be isolated from an Ophiocordyceps-associated fungus, Clonostachys rogersoniana. Rogersonin E downregulates the expression of PD-L1 protein in MDA-MB-231 and A549 cells.
    Rogersonin E
  • HY-169364
    2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc
    		Ligand
    2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc is the PD-L1 ligand-linker conjugate part of AUTAC PD-L1 degrader-3 (HY-169363). 2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc can be utilized in AUTAC synthesis.
    2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc
  • HY-P1610
    Asudemotide
    		Inducer
    Asudemotide (S-588410) is a peptide of human DEP domain-containing protein 1A. Asudemotide is an immunostimulant. Asudemotide has a sequence of H-Glu-Tyr-Tyr-Glu-Leu-Phe-Val-Asn-Ile-OH. Asudemotide induces a tumor immune response in esophageal cancer. .
    Asudemotide
  • HY-P990740
    Fanastomig
    Fanastomig is an anti-PDCD1/LAG3 monoclonal antibody.
    Fanastomig
  • HY-P99048A
    Sintilimab (Anti-PD-1)
    		Inhibitor
    Sintilimab (Anti-PD-1) (IBI308 (Anti-PD-1)) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a KD value of 74 pM. Sintilimab (Anti-PD-1) blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab (Anti-PD-1) combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab (Anti-PD-1) can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer.
    Sintilimab (Anti-PD-1)
  • HY-P5276
    Human membrane-bound PD-L1 polypeptide
    Human membrane-bound PD-L1 polypeptide can be used as an antigen to induce PD-L1 antibody production.
    Human membrane-bound PD-L1 polypeptide
  • HY-144447
    PD-1/PD-L1-IN-17
    		Inhibitor
    PD-1/PD-L1-IN-17 (Compound P20) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 26.8 nM. PD-1/PD-L1-IN-17 is a promising lead compound for the development of inhibitors of the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-17 has the potential for the research of cancer diseases.
    PD-1/PD-L1-IN-17
  • HY-168086
    LSD1-IN-35
    		Inhibitor
    LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction.
    LSD1-IN-35
  • HY-P990778
    Xirestomig
    Xirestomig is an anti-TNFRSF9/CD274 monoclonal antibody.
    Xirestomig
  • HY-156150
    CYP51/PD-L1-IN-2
    		Inhibitor
    CYP51/PD-L1-IN-2 (compound L20) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-2 is a dual inhibitor of CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.017 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-2 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death.
    CYP51/PD-L1-IN-2
  • HY-P991518
    IBI-322
    		Inhibitor
    IBI-322 is a bispecific antibody targeting PD-L1 and CD47. IBI-322 attenuates CD47 activity in monovalent binding and blockes PD-L1 activity in bivalent binding. IBI-322 selectively binds to CD47+PD-L1+ tumor cells, effectively inhibits CD47-SIRPα signal and triggered strong tumor cell phagocytosis in vitro.
    IBI-322
Cat. No. Product Name / Synonyms Application Reactivity