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, also known as KAI-9803, is a synthetic peptide inhibitor specifically designed to target protein kinase C delta (PKCδ), an enzyme implicated in a variety of intracellular signaling pathways. As a cell-permeable peptide, Delcasertib exhibits high selectivity and affinity for PKCδ, making it a valuable research tool for dissecting the complex roles of this kinase in cellular physiology. Researchers have utilized this compound to investigate the modulation of signal transduction mechanisms in multiple biological contexts, particularly those involving stress response, apoptosis, and inflammation. Due to its potent inhibitory action, Delcasertib serves as a molecular probe to unravel the downstream effects of PKCδ activation or suppression, thereby facilitating a deeper understanding of cellular regulation and pathophysiological processes.
Signal Transduction Studies: Delcasertib is widely employed in signal transduction research to elucidate the specific functions of PKCδ within cellular signaling cascades. By selectively inhibiting this kinase, scientists can delineate its role in the phosphorylation of downstream targets, identify cross-talk with other signaling pathways, and uncover regulatory checkpoints that govern cell fate decisions. This peptide tool enables precise manipulation of PKCδ activity, providing insights into its contribution to cellular responses under various experimental conditions.
Apoptosis Research: The use of KAI-9803 in apoptosis research has proven instrumental in clarifying the involvement of PKCδ in programmed cell death. By inhibiting PKCδ, researchers can assess its influence on the activation of caspases, mitochondrial membrane potential changes, and the release of pro-apoptotic factors. These studies are critical for differentiating the pro-survival and pro-apoptotic functions of PKC isoforms and for identifying potential molecular targets within cell death pathways.
Cardiovascular Pathophysiology: In the field of cardiovascular research, Delcasertib has been utilized to explore the role of PKCδ in ischemia-reperfusion injury models, where oxidative stress and inflammation are prominent. By modulating PKCδ activity, investigators can evaluate its impact on cardiomyocyte survival, contractility, and the regulation of protective signaling mechanisms. These findings contribute to a broader understanding of the molecular events that underlie cardiac tissue damage and repair, offering new perspectives on the modulation of heart function at the cellular level.
Inflammatory Signaling: Delcasertib's ability to specifically inhibit PKCδ has facilitated studies on inflammatory signaling pathways. Researchers employ this compound to investigate the regulation of cytokine production, leukocyte activation, and vascular permeability in response to inflammatory stimuli. By dissecting the signaling networks orchestrated by PKCδ, scientists can better understand the mechanisms that drive inflammation and identify molecular checkpoints amenable to therapeutic intervention in preclinical models.
Neurobiology and Neuroprotection: The application of KAI-9803 extends to neurobiological studies, where it is used to probe the role of PKCδ in neuronal injury, synaptic plasticity, and neuroprotection. Inhibition of PKCδ activity allows researchers to assess its involvement in neuronal apoptosis, oxidative stress responses, and the modulation of neurotrophic factors. These investigations provide valuable information on the molecular determinants of neuronal survival and adaptation, supporting the exploration of new strategies for protecting neural tissue from various insults.
Delcasertib continues to support a wide range of research applications due to its specificity and effectiveness as a PKCδ inhibitor. Its versatility has made it indispensable in studies spanning cell signaling, apoptosis, cardiovascular biology, inflammation, and neurobiology. By enabling precise modulation of PKCδ activity, this peptide compound empowers scientists to unravel intricate molecular mechanisms and advance the understanding of complex biological systems. As research progresses, Delcasertib remains a critical tool for exploring the diverse roles of protein kinase C delta in health and disease models, driving innovation and discovery across multiple scientific disciplines.
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