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-169434
    LTB
    		Inhibitor
    LTB is a prodrug formed by coupling glycolysis inhibitor (Lonidamine (HY-B0486)) with PD1/PDL1 blocker (BMS-1 (HY-19991)) by thioketal linkage. LTB can further encapsulate photosensitizer chlorine e6 (Ce6) (HY-13594) to construct a co-delivery photodynamic nanoplatform (LTB-6 NPs) by self-assembly.
    LTB
  • HY-144443
    PD-1/PD-L1-IN-16
    		Inhibitor
    PD-1/PD-L1-IN-16 (Compound M23) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 53.2 nM. PD-1/PD-L1-IN-16 has the potential for the research of tumor immunoresearch.
    PD-1/PD-L1-IN-16
  • HY-173070
    TLR7 agonist 29
    		Activator
    TLR7 agonist 29 (Compound 1) is the agonist for TLR7 with an EC50 of 5.2 nM for human TLR7 (EC50 for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC.
    TLR7 agonist 29
  • HY-163534
    PD-1/PD-L1-IN-43
    		Inhibitor
    PD-1/PD-L1-IN-43 (compound Z13) is a small-molecule inhibitors targeting the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-43 exhibites potent in vivo antitumor efficacy against B16-F10 melanoma. PD-1/PD-L1-IN-43 inhibits tumor growth by blocking the interaction between PD-1 and PD-L1. PD-1/PD-L1-IN-43 can be used in anti-tumor studies.
    PD-1/PD-L1-IN-43
  • HY-145771
    PD-1/PD-L1-IN-20
    		Inhibitor
    PD-1/PD-L1-IN-20 (Example 21) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-20 blocks PD-1/PD-L1 with the IC50 of 5.29 nM. PD-1/PD-L1-IN-20 can be used for the research of cancers, infectious diseases and autoimmune diseases.
    PD-1/PD-L1-IN-20
  • HY-162463
    Ir-UA
    		Activator
    Ir-UA is an usnic acid-derived iridium(III) complex that enhances PD-L1 expression and converts "cold tumors" into "hot tumors." Ir-UA stimulates PD-L1 expression by explicitly regulating the PD-L1 transcription factor.
    Ir-UA
  • 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-P99619
    Finotonlimab
    		Inhibitor
    Finotonlimab (SCT-I10A) is a recombinant humanised IgG PD-1 antibody. Finotonlimab has the potential for solid tumors or lymphomas research.
    Finotonlimab
  • 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-P99668
    Iparomlimab
    		Inhibitor
    Iparomlimab is an anti-human PD-1/CD279/PDCD1 IgG4κ antibody. Iparomlimab also targets to human monoclonal PSB103 γ4-chain, disulfided with human monoclonal PSB103 κ-chain to form a dimer. Iparomlimab can be used for Oncology research.
    Iparomlimab
  • 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-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)
Cat. No. Product Name / Synonyms Application Reactivity