Delcasertib,a Novel δ-Protein Kinase C Inhibitor,is composed of a selective δ-protein kinase C (δPKC) inhibitor peptide conjugated reversibly to the cell-penetrating peptide via a disulfide bond.
CAT No: 10-101-143
CAS No:949100-39-4
Synonyms/Alias:DELCASERTIB;949100-39-4;Delcasertib [USAN:INN];UNII-5G7N7E908H;5G7N7E908H;KAI-9803;BMS-875944;Delcasertib [USAN];delcasertibum;DELCASERTIB [INN];DELCASERTIB [WHO-DD];AKOS040733515;CS-9803;TS-07824;KAI-9803; BMS-875944;CYS-TYR-GLY-ARG-LYS-LYS-ARG-ARG-GLN-ARG-ARG-ARG CYS-SER-PHE-ASN-SER-TYR-GLU-LEU-GLY-SER-LEU 1-1'-DISULFIDE;L-Arginine, L-cysteinyl-L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L- glutaminyl-L-arginyl-L-arginyl-, (1->1')-disulfide with L-cysteinyl-L-seryl-L-phenylalanyl-L- asparaginyl-L-seryl-L-tyrosyl-L-alpha-glutamyl-L-leucylglycyl-L-seryl-L-leucine;L-Cysteinyl-L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L-glutaminyl-L- arginyl-L-arginyl-L-arginine (1->1')-disulfide with L-cysteinyl-L-seryl-L-phenylalanyl-L- asparaginyl-L-seryl-L-tyrosyl-L-alpha-glutamyl-L-leucylglycyl-L-seryl-L-leucine;
Delcasertib is a synthetic small-molecule inhibitor known for its specificity toward protein kinase C delta (PKCδ), a key isoform within the protein kinase C family involved in diverse signal transduction pathways. As a non-peptidic compound, Delcasertib has garnered significant attention in biochemical and cellular research due to its ability to modulate phosphorylation events critical to cellular stress response, apoptosis, and signal integration. By selectively targeting PKCδ, it provides researchers with a powerful tool to dissect the molecular mechanisms underlying kinase-mediated processes and to elucidate the functional roles of PKCδ in various physiological and pathophysiological contexts.
Signal Transduction Research: Delcasertib is widely employed in studies investigating the intricate signaling networks regulated by PKCδ. Its selective inhibition enables precise interrogation of PKCδ-dependent phosphorylation cascades, allowing scientists to map downstream effectors and to distinguish PKCδ-mediated events from those controlled by other PKC isoforms. Such studies are instrumental in advancing the understanding of how PKCδ integrates external stimuli to modulate cell fate decisions, including proliferation, differentiation, and programmed cell death.
Apoptosis and Cell Death Mechanisms: The compound serves as a critical reagent in research focused on apoptosis and necrosis, where PKCδ is recognized as a central mediator. By blocking PKCδ activity, Delcasertib facilitates the delineation of signaling pathways that govern mitochondrial dysfunction, caspase activation, and DNA fragmentation. This application is particularly valuable in exploring the molecular basis of cell injury, stress-induced apoptosis, and the role of PKCδ in cellular responses to oxidative damage or DNA-damaging agents.
Cardiovascular Signal Modulation: In the context of cardiovascular research, Delcasertib is utilized to investigate the signaling events associated with ischemia-reperfusion injury and myocardial stress responses. PKCδ has been implicated in the regulation of cardiomyocyte survival and contractility under stress conditions. The use of this inhibitor allows researchers to clarify the contribution of PKCδ activity to cardiac signaling networks, providing mechanistic insights into the cellular adaptations that occur during hypoxia, reperfusion, and oxidative challenge.
Cellular Stress and Inflammatory Pathways: Delcasertib is also applied in studies examining the cellular response to inflammatory stimuli and environmental stressors. By modulating PKCδ activity, researchers can evaluate its role in the activation of transcription factors, cytokine production, and the regulation of stress-activated protein kinases. Such investigations contribute to a broader understanding of how PKCδ influences inflammation, immune cell activation, and adaptation to cellular stress, thereby supporting the development of new hypotheses regarding the regulation of inflammatory signaling.
Phosphorylation Assay Development: The specificity of Delcasertib for PKCδ makes it a valuable control in the development and validation of in vitro kinase assays. It is frequently used to confirm assay selectivity, to benchmark the inhibitory effects of novel compounds, and to facilitate the identification of PKCδ substrates. Its use in assay optimization ensures that observed phosphorylation events are attributable to PKCδ, enhancing the reliability and interpretability of experimental data in high-throughput screening and mechanistic enzymology studies.
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