PD-1/PD-L1 Inhibitor is a macrocyclic inhibitor of PD-1/PD-L1 interaction with an IC50 of 5.6 nM. In vitro ab231310 is capable of inhibiting the interaction of PD-L1 with PD-1 and with CD80. It has highly efficacious binding to PD-L1 and promotes enhanced T cell functional activity.
CAT No: R1891
CAS No:1629654-95-0
Synonyms/Alias:PD-1/PD-L1 Inhibitor 3;1629654-95-0;EQC65495;(3S,6S,12S,15S,18S,21S,24S,27S,30R,39S,42S,47aS)-3-((1H-imidazol-5-yl)methyl)-12,18-bis((1H-indol-3-yl)methyl)-N,42-bis(2-amino-2-oxoethyl)-36-benzyl-21,24-dibutyl-27-(3-guanidinopropyl)-15-(hydroxymethyl)-6-isobutyl-8,20,23,38,39-pentamethyl-1,4,7,1;
Chemical Name:(3S,6S,12S,15S,18S,21S,24S,27S,30R,39S,42S,47aS)-3-((1H-imidazol-5-yl)methyl)-12,18-bis((1H-indol-3-yl)methyl)-N,42-bis(2-amino-2-oxoethyl)-36-benzyl-21,24-dibutyl-27-(3-guanidinopropyl)-15-(hydroxymethyl)-6-isobutyl-8,20,23,38,39-pentamethyl-1,4,7,10,13,
PD-1/PD-L1 Inhibitor 3 is a synthetic small molecule designed to modulate immune checkpoint pathways by selectively disrupting the interaction between programmed cell death protein 1 (PD-1) and its ligand PD-L1. As a member of the immune checkpoint inhibitor class, it plays a crucial role in immunological research by enabling detailed studies of T cell activation, immune tolerance, and tumor immunology. Its biochemical structure allows for precise interference with the PD-1/PD-L1 axis, making it an essential reagent for elucidating the molecular mechanisms underlying immune evasion and for exploring new frontiers in immunomodulation. The compound is widely recognized for its value in research settings focused on immune signaling, cellular assays, and the development of novel immunotherapeutic strategies.
Immuno-oncology research: As an established PD-1/PD-L1 pathway antagonist, this inhibitor is routinely employed in immuno-oncology studies to investigate the cellular and molecular basis of immune checkpoint regulation. Researchers utilize it to mimic or block the inhibitory signals that normally dampen T cell responses within the tumor microenvironment. By preventing PD-1 from binding to PD-L1, the compound facilitates the reactivation of effector T cells, allowing for robust analyses of anti-tumor immunity in both in vitro and ex vivo models. Such studies are integral to understanding mechanisms of immune escape and identifying potential targets for next-generation immunotherapies.
Cell signaling pathway analysis: The inhibitor is a versatile tool for dissecting the downstream signaling cascades initiated by PD-1/PD-L1 engagement. Its application in cell-based assays enables the precise assessment of phosphorylation events, transcription factor activity, and cytokine production that result from checkpoint blockade. By modulating these pathways, the compound allows scientists to define the contributions of PD-1/PD-L1 signaling to immune cell function, tolerance, and exhaustion, providing critical insights into the regulation of adaptive immunity.
Drug discovery and screening: In the context of high-throughput screening and drug development, PD-1/PD-L1 Inhibitor 3 serves as a reference compound or positive control for evaluating the efficacy of novel checkpoint inhibitors. Its well-characterized activity profile makes it suitable for benchmarking candidate molecules in biochemical and cellular assays. This application supports the identification and optimization of new small molecules or biologics targeting the PD-1/PD-L1 axis, thereby accelerating the preclinical evaluation of potential immunomodulatory agents.
Mechanistic studies of immune regulation: The compound is instrumental in mechanistic studies aimed at unraveling the complexities of immune regulation in health and disease. By selectively inhibiting PD-1/PD-L1 interactions, it enables researchers to delineate the specific contributions of this pathway to peripheral tolerance, autoimmunity, and immune surveillance. Such investigations are vital for mapping the interplay between co-inhibitory and co-stimulatory signals in various immunological contexts, enhancing our understanding of immune homeostasis.
Assay development and validation: PD-1/PD-L1 Inhibitor 3 is frequently employed in the development and validation of novel immunoassays, including flow cytometry-based detection of checkpoint expression and functional assays measuring T cell activation or cytokine release. Its defined mode of action and reproducible effects make it an ideal standard for calibrating assay sensitivity, establishing dynamic ranges, and ensuring the reliability of experimental readouts. These capabilities are essential for laboratories seeking to implement robust, quantitative methods for immune checkpoint analysis in basic and applied research.
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