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

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-157055
    PD-1-IN-25
    Inhibitor
    PD-1-IN-25 (compound 43) is a potent PD-1/PD-L1 interaction inhibitor with an IC50 value of 10.2 nM in the HTRF assay. PD-1-IN-25 can promote CD8+ T cell activation through inhibiting PD-1/PD-L1 cellular signaling. PD-1-IN-25 delays the tumor growth.
    PD-1-IN-25
  • HY-120646
    BMS-242
    Inhibitor
    BMS-242 is a small molecule PD-1/PD-L1 inhibitor with the activity of inhibiting the PD-1/PD-L1 interaction. BMS-242 can bind to the hydrophobic channel pocket between PD-L1 molecules, inhibit the PD-1/PD-L1 immune checkpoint pathway, and provide a new way for cancer inhibition.
    BMS-242
  • HY-159101
    EP26
    Inhibitor
    EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma.
    EP26
  • HY-144649
    PD-1/PD-L1-IN-24
    Inhibitor
    PD-1/PD-L1-IN-24 is a highly potent PD-1/PD-L1 inhibitor with IC50 value of 1.57 nM. PD-1/PD-L1-IN-24 can restore T-cell function at the cellular level by significantly elevating the IFN-γ level. PD-1/PD-L1-IN-24 has low toxicity on the PBMCs.
    PD-1/PD-L1-IN-24
  • HY-145772
    PD-1/PD-L1-IN-21
    Inhibitor
    PD-1/PD-L1-IN-21 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-21 blocks PD-1/PD-L1 with the IC50 of 4.99 μM. PD-1/PD-L1-IN-21 can be used for the research of cancers, infectious diseases and autoimmune diseases.
    PD-1/PD-L1-IN-21
  • HY-P990088
    Sotiburafusp alfa
    Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor.
    Sotiburafusp alfa
  • HY-156151
    CYP51/PD-L1-IN-3
    Inhibitor
    CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 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-3
  • HY-P10826
    PD-1/PD-L1 inhibitory peptide C8
    Inhibitor
    PD-1/PD-L1 inhibitory peptide C8 is inhibits PD-1/PD-L1 interaction, promotes the activation of CD8+ and CD4+ T cells, and increases the IFN-γ secretion. PD-1/PD-L1 inhibitory peptide C8 exhibits antitumor efficacy in mouse model.
    PD-1/PD-L1 inhibitory peptide C8
  • HY-144497
    HE-S2
    Inhibitor
    HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity.
    HE-S2
  • HY-169190
    PD-1/PD-L1-IN-53
    Inhibitor
    PD-1/PD-L1-IN-53 (compound B3) is an inhibitor targeting PD-1/PD-L1 and VISTA signaling pathways. PD-1/PD-L1-IN-53 can be used in anti-cancer research.
    PD-1/PD-L1-IN-53
  • HY-150617A
    (Rac)-Lartesertib
    Control
    (Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity.
    (Rac)-Lartesertib
  • HY-170793
    PD-L1/VISTA-IN-1
    Inhibitor
    PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual-target inhibitor of PD-L1 and VISTA. PD-L1/VISTA-IN-1 can block the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), thereby reactivating T cells. PD-L1/VISTA-IN-1 has anti-tumor activity.
    PD-L1/VISTA-IN-1
  • HY-P990704
    Rilvegostomig
    99.00%
    Rilvegostomig is an anti-PDCD1/TIGIT human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Rilvegostomig
  • HY-161605
    HBV/HDV-IN-2
    Inhibitor
    HBV/HDV-IN-2 (Compd 143) is a HBV, HDV and PD-1/PD-L1 inhibitor, with an EC50 of 35 nM for T cell activation.
    HBV/HDV-IN-2
  • HY-P990738
    Enristomig
    Enristomig is an anti-TNFRSF9/CD274 monoclonal antibody.
    Enristomig
  • HY-P990700
    Tobemstomig
    Tobemstomig is an anti-PDCD1/LAG3 human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Tobemstomig
  • HY-19991A
    (Rac)-BMS-1
    Inhibitor
    (Rac)-BMS-1 is a racemate of BMS-1 (HY-19991A). (Rac)-BMS-1 can be used as a target protein ligand to synthesize D5B PROTAC (HY-169392).
    (Rac)-BMS-1
  • HY-172809
    LSD1-IN-42
    Inhibitor
    LSD1-IN-42 (Compound 7ae) is an orally active LSD1 inhibitor that potently inhibits LSD1 activity (IC50 = 0.08 μM). LSD1-IN-42 downregulates PD-L1 expression and enhances T cell-mediated tumor killing effects. LSD1-IN-42 demonstrates significant anti-gastric cancer activity by inhibiting tumor cell invasion and migration.
    LSD1-IN-42
  • HY-161713
    PD-1/PD-L1-IN-45
    Inhibitor
    PD-1/PD-L1-IN-45 (Compound 2) is an inhibitor for PD-1/PD-L1 Interaction with EC50 of 21.8 nM.
    PD-1/PD-L1-IN-45
  • HY-157569
    PD1-PDL1-IN 2
    PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1 inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β.
    PD1-PDL1-IN 2
Cat. No. Product Name / Synonyms Application Reactivity