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-162357
    PD-L1-IN-5
    		Inhibitor
    PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor, with the IC50 value of 785.6 nM. PD-L1-IN-5 has anti-tumor activity in vivo.
    PD-L1-IN-5
  • HY-155115
    LSD1-IN-27
    		Inhibitor 98.88%
    LSD1-IN-27 is an orally active LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer.
    LSD1-IN-27
  • HY-N0460R
    1-Caffeoylquinic acid (Standard)
    		Inhibitor
    1-Caffeoylquinic acid (Standard) is the analytical standard of 1-Caffeoylquinic acid. This product is intended for research and analytical applications. 1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.007 μM. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid is the inhibitor for PD-1/PD-L1.
    1-Caffeoylquinic acid (Standard)
  • HY-159892
    PD-1/PD-L1-IN-54
    		Inhibitor
    PD-1/PD-L1-IN-54 (Compound 6) is a moderately affinic PD-1/PD-L1 inhibitor (KD: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC50: 88.6 μM). PD-1/PD-L1-IN-54 inhibits PD-1/PD-L1 interactions and shows anticancer activity by activating CD8+ T cells, upregulating PD-1 expression, and increasing secretion of IFN-γ and IL-2. PD-1/PD-L1-IN-54 inhibits cancer cell proliferation and promotes apoptosis. PD-1/PD-L1-IN-54 also regulates T cell immunity through the PI3K/Akt pathway correlated with PD-1/PD-L1.
    PD-1/PD-L1-IN-54
  • HY-144746
    PD-1/PD-L1-IN-26
    		Inhibitor
    PD-1/PD-L1-IN-26 (Compound II-14) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 0.0380 μM. PD-1/PD-L1-IN-26 activates the immune microenvironment by promoting the infiltration of CD4+ T cells into tumor tissues. PD-1/PD-L1-IN-26 has the potential for the research of cancer diseases.
    PD-1/PD-L1-IN-26
  • HY-163844
    PD-1/PD-L1-IN-49
    		Inhibitor
    PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1, with the IC50 of 77 nM. PD-1/PD-L1-IN-49 activates Jurkat T cells, reflecting successful blockade of the PD-1/PD-L1 immune checkpoint.
    PD-1/PD-L1-IN-49
  • HY-P991354
    GR-1405
    		Antagonist
    GR-1405 is a human monoclonal antibody (mAb) targeting B7-H1/PD-L1/CD274. GR-1405 enhances cytotoxic T lymphocyte (CTL)-mediated antitumor immune responses against PD-L1-expressing tumor cells. GR-1405 can be used in Lymphoma and Solid tumours research.
    GR-1405
  • HY-157811
    PD-1/PD-L1-IN-40
    		Inhibitor
    PD-1/PD-L1-IN-40 (Compound EP16) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-40 inhibits the generation of exosomal PD-L1 with IC50 = 0.108 μM. PD-1/PD-L1-IN-40 can serve as a leading compound for exosomal PD-L1 abrogation. PD-1/PD-L1-IN-40 can be used for the research of cancer.
    PD-1/PD-L1-IN-40
  • HY-P991151
    Opamtistomig
    		Inhibitor
    Opamtistomig is a humanized immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody targeting human programmed death ligand 1 (PD-L1), CD274 and tumor necrosis factor receptor superfamily member 9 (TNFRSF9). Opamtistomig is promising for research of various solid tumors and hematological malignancies.
    Opamtistomig
  • HY-175014
    LGT-1
    		Ligand
    LGT-1 is a PD-L1 ligand. LGT-1 labeled with 18F has an excellent specific uptake in B16-F10 tumor cells, and shows a high tumor uptake but a low liver uptake with good stability in B16-F10 tumor-bearing mice model. LGT-1 can be used as a radiotracer for PET imaging of PD-L1 expression in tumors.
    LGT-1
  • HY-P99106
    Acrixolimab
    		Inhibitor
    Acrixolimab a humanized IgG4-κ antibody, targeting to PD-1.
    Acrixolimab
  • HY-P10838
    PL120131
    		Inhibitor
    PL120131 is a PD-1/PD-L1 inhibitory peptide that can interfere with the interaction of PD-1/PD-L1 by binding to PD-1. PL120131 is capable of inhibiting the PD-1-mediated apoptotic signaling pathway, protecting Jurkat cells and primary lymphocytes from apoptosis. PL120131 aids in the antitumor activity of cytotoxic T lymphocytes (CTLs).
    PL120131
  • HY-162972
    PROTAC PD-L1 degrader-2
    		Degrader
    PROTAC PD-L1 degrader-2 (Compound 9i) is a PROTAC degrader for PD-L1, that inhibits PD-L1 with an IC50 of 197.4 nM and exhibits an affinity with PD-L1 with a Kd of 301 nM. PROTAC PD-L1 degrader-2 promotes the internalization of PD-L1 on the cell membrane, and induces PD-L1 degradation via the synergistic effect of the proteasome and lysosomal pathways. PROTAC PD-L1 degrader-2 can activate the immune system, and exhibits antitumor efficacy in MC38 C57BL/6 mouse model.
    PROTAC PD-L1 degrader-2
  • 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-173558
    PD-L1/HDAC3-IN-1
    		Inhibitor
    PD-L1/HDAC3-IN-1 (PH3) is a dual PD-L1/HDAC3 Inhibitor with IC50 values of 89.4 nM and 107 nM for PD-1/PD-L1 and HDAC3, respectively. PD-L1/HDAC3-IN-1 induces cell apoptosis and arrests cell cycle at G0/G1 phase. PD-L1/HDAC3-IN-1 shows anticancer activity both in vivo and in vitro.
    PD-L1/HDAC3-IN-1
Cat. No. Product Name / Synonyms Application Reactivity