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-162343
    PD-1/PD-L1-IN-41
    		Inhibitor
    PD-1/ PD-L1-in-41 (Compound 5c) is a PD-L1 and PD-1 inhibitor with IC50 value of 10.2 nM.
    PD-1/PD-L1-IN-41
  • HY-161604
    HBV/HDV-IN-1
    		Inhibitor
    HBV/HDV-IN-1 (Compd 122) is a HBV, HDV and PD-1/PD-L1 inhibitor, with EC50 values of 8 nM for T cell activation and 35 nM for PD-L1 internalization.
    HBV/HDV-IN-1
  • HY-P99100A
    Visugromab (Powder)
    Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).
    Visugromab (Powder)
  • HY-N12537A
    (2R,3S)-PD-1/PD-L1-IN-38
    		Inhibitor
    (2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8+T cells and inhibits the signal transduction of PD-1/PD-L1.
    (2R,3S)-PD-1/PD-L1-IN-38
  • HY-N0242R
    Fraxinellone (Standard)
    		Inhibitor
    Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
    Fraxinellone (Standard)
  • HY-P991113
    Abazistobart
    		Inhibitor
    Abazistobart is an immunostimulant and antineoplastic agent targeting the programmed cell death protein 1 (PDCD1). Abazistobart is a chimeric and humanized monoclonal antibody that specifically binds to PDCD1 to block the relevant signaling pathway, thereby activating the immune system and exerting antineoplastic activity. Abazistobart is promising for research of cancers.
    Abazistobart
  • HY-168081
    PD-1/PD-L1-IN-52
    		Inhibitor
    PD-1/PD-L1-IN-52 (Compound III-5) is an orally active PD-1/PD-L1 inhibitor that blocks the interaction between PD-1 and PD-L1, with an IC50 of 109.9 nM. PD-1/PD-L1-IN-52 exhibits antitumor activity in a C57BL/6 mouse xenograft model implanted with human PD-1-expressing MC38 colon cancer cells, with a TGI of 49.6%.
    PD-1/PD-L1-IN-52
  • HY-162643
    Antitumor agent-169
    		Inhibitor
    Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics.
    Antitumor agent-169
  • HY-W009762S1
    L-Lysine6-13C dihydrochloride
    		Inhibitor
    L-Lysine6-13C (dihydrochloride) is a 13C-labeled L-Lysine dihydrochloride.
    L-Lysine6-<sup>13</sup>C dihydrochloride
  • HY-149356
    PD-1/PD-L1-IN-31
    		Inhibitor
    PD-1/PD-L1-IN-31 is a PD-1/PD-L1 inhibitor (IC50=2.2 nM). PD-1/PD-L1-IN-31 promotes secretion of the IFN-γ, and induces immune activity of peripheral blood mononuclear cells (PBMCs) to inhibits tumor cells.
    PD-1/PD-L1-IN-31
  • 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-P991449
    LY3415244
    		Inhibitor
    LY3415244 is a human bispecific antibody (bsAb) targeting B7-H1/PD-L1/CD274 & TIM-3/HAVCR2/CD366. LY3415244 can be used in advanced solid tumors research.
    LY3415244
  • 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-P991356
    FAZ-053
    		Antagonist
    FAZ-053 is a human monoclonal antibody (mAb) targeting B7-H1/PD-L1/CD274. FAZ-053 inhibits the interaction of PD-L1 with PD-1 and B7-1 on monocytes, dendritic cells, and B cells. FAZ-053 enhances interleukin 2 production. FAZ-053 can be used in advanced alveolar soft tissue sarcoma (ASPS), chordoma, and triple-negative breast cancer research.
    FAZ-053
Cat. No. Product Name / Synonyms Application Reactivity