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

PD-1/PD-L1

PD-1/Programmed death-ligand 1

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-162644
    Antitumor agent-170
    Inhibitor
    Antitumor agent-170 (Compound C6) exhibits inhibitory activities against PD-1/PD-L1 interaction and PARP7, with IC50 of 0.342 μM and 7.05 nM. Antitumor agent-170 exhibits a high affinity to human PD-L1, with a Ki of 9.31 nM. Antitumor agent-170 restores the T cell function and increases IFN-γ secretion. Antitumor agent-170 exhibits antitumor efficacy against melanoma in mouse models and good pharmacokinetic characteristics.
    Antitumor agent-170
  • HY-P99679
    Izuralimab
    Inhibitor
    Izuralimab is a bispecific IgG1 antibody targeting inducible T-cell costimulator (ICOS/CD278) and PD-1.
    Izuralimab
  • HY-161518
    PD-1/PD-L1-IN-44
    Inhibitor
    PD-1/PD-L1-IN-44 (Compound 22) selectively inhibits PD-1/PD-L1 proteins (IC50=1.21 nM). PD-1/PD-L1-IN-44 inhibits tumor growth without toxicity in animal models and increases CD8+ cell infiltration.
    PD-1/PD-L1-IN-44
  • HY-167840
    IMMH-010 maleate
    Inhibitor
    IMMH-010 maleate is a prodrug that serves as a novel PD-L1 inhibitor, exhibiting potential antitumor activity for the treatment of neurological disorders and advanced malignant solid tumors. IMMH-010 maleate is rapidly converted to its active form, YPD-29B, following oral administration. IMMH-010 maleate is poised for advancing research in the field of PD-L1 inhibitors and related therapeutic applications.
    IMMH-010 maleate
  • HY-P99723
    Manelimab
    Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 (PD-L1).
    Manelimab
  • HY-172396
    PD-L1/VISTA-IN-2
    Inhibitor
    PD-L1/VISTA-IN-2 (Compound S8) is an orally active bifunctional PD-L1/VISTA inhibitor with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. PD-L1/VISTA-IN-2 can activate the tumor immune microenvironment and exert anti-cancer effects.
    PD-L1/VISTA-IN-2
  • HY-P990169
    Anti-Mouse/Human phosphorylated PD-1/CD279 Antibody (407.6G12)
    Inhibitor
    Anti-Mouse/Human phosphorylated PD-1/CD279 Antibody (407.6G12) is a mouse-derived IgG2a, κ type antibody inhibitor, targeting to mouse/human phosphorylated PD-1/CD279.
    Anti-Mouse/Human phosphorylated PD-1/CD279 Antibody (407.6G12)
  • HY-156085
    LP23
    Inhibitor
    LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC50: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg).
    LP23
  • HY-P990824
    Anti-Mouse PD-1 Antibody (J43)
    Inhibitor
    Anti-Mouse PD-1 Antibody (J43) is a kind of Armenian hamster IgG in vivo mouse antibody, targeting to PD-1. The recommend isotype control of Anti-Mouse PD-1 Antibody (J43): Armenian hamster IgG, Isotype Control (HY-P990305).
    Anti-Mouse PD-1 Antibody (J43)
  • HY-156149
    CYP51/PD-L1-IN-1
    Inhibitor
    CYP51/PD-L1-IN-1 (compound L11) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-1 is a dual inhibitor of CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-1 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-1
  • 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 (Compound 5ac) is a 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-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-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-168530
    PDL1 degrader-1
    Degrader
    PDL1 degrader-1 (compound PMT-O9-1A) is a potent PD-L1 degrader. PDL1 degrader-1 decreases the protein expression of PD-L1. PDL1 degrader-1 shows cytotoxicity. PDL1 degrader-1 shows anticancer activity.
    PDL1 degrader-1
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity