Balixafortide is an orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Balixafortide binds to the chemokine receptor CXCR4, thereby preventing the binding of stromal-derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation. This may induce the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the blood.
CAT No: R1869
CAS No:1051366-32-5
Synonyms/Alias:Balixafortide;1051366-32-5;POL6326;Balixafortide [INN];Balixafortide [USAN];PRC974M49B;POL-6326;Cyclo(L-alanyl-L-cysteinyl-L-seryl-L-alanyl-D-prolyl-(2S)-2,4-diaminobutanoyl-L-arginyl-L-tyrosyl-L-cysteinyl-L-tyrosyl-L-glutaminyl-L-lysyl-D-prolyl-L-prolyl-L-tyrosyl-L-histidyl), cyclic (2->9)-disulfide;Ala-cys-ser-ala-pro-arg-tyr-cys-tyr-gln-lys-pro-pro-tyr-his cyclic (2->9)-disulfide;balixafortidum;11-Dideuterolinoleic acid;Balixafortide(POL6326);Balixafortide [USAN:INN];UNII-PRC974M49B;BALIXAFORTIDE [WHO-DD];GTPL11587;POL 6326;WHO 9915;DA-61485;
Chemical Name:Cyclo(L-alanyl-L-cysteinyl-L-seryl-L-alanyl-D-prolyl-(2S)-2,4-diaminobutanoyl-L-arginyl-L-tyrosyl-L-cysteinyl-L-tyrosyl-L-glutaminyl-L-lysyl-D-prolyl-L-prolyl-L-tyrosyl-L-histidyl), cyclic (2->9)-disulfide
Balixafortide is a synthetic cyclic peptide known for its potent and selective antagonism of the CXC chemokine receptor 4 (CXCR4). As a highly characterized peptide compound, it is widely recognized for its ability to modulate chemokine signaling pathways, which play a critical role in cellular migration, immune cell trafficking, and various physiological and pathological processes. Due to its specificity and robust activity, Balixafortide has become a valuable research tool for investigating CXCR4-mediated cellular mechanisms, facilitating studies in immunology, oncology, and cell biology. Its unique structure and receptor affinity offer researchers a reliable means to dissect chemokine receptor function and explore the complexities of cell signaling networks.
Receptor Antagonism Studies: As a selective CXCR4 antagonist, Balixafortide is extensively utilized in receptor-ligand interaction studies to elucidate the molecular mechanisms governing chemokine receptor signaling. By competitively inhibiting CXCR4, it enables researchers to dissect the downstream effects of receptor blockade, providing insights into the roles of CXCR4 in cell migration, adhesion, and signal transduction. These studies are instrumental in understanding the contribution of chemokine receptors to physiological processes such as hematopoiesis, immune surveillance, and tissue repair.
Cancer Cell Migration Research: The compound is frequently employed in in vitro and in vivo models to investigate the role of CXCR4 in tumor cell migration, invasion, and metastasis. By disrupting the CXCL12/CXCR4 signaling axis, Balixafortide allows scientists to model and quantify the impact of chemokine receptor inhibition on cancer cell behavior. This application is particularly relevant in studies aiming to unravel the molecular determinants of metastatic spread and to identify potential molecular targets for modulating tumor microenvironments.
Immunology and Inflammation Studies: Balixafortide serves as a critical tool in immunological research focused on leukocyte trafficking and inflammatory responses. By blocking CXCR4-mediated chemotaxis, it provides a means to assess the migration patterns of immune cells under various experimental conditions. This function is essential for delineating the mechanisms of immune cell recruitment to sites of inflammation, as well as for exploring the interplay between chemokine gradients and immune regulation in both normal and pathological states.
Stem Cell Mobilization Investigations: Research on hematopoietic stem and progenitor cell trafficking often employs Balixafortide to interrogate the regulatory role of CXCR4 in stem cell retention and mobilization. By inhibiting receptor function, the compound facilitates studies on the release and movement of stem cells from the bone marrow into peripheral circulation. Such investigations are fundamental for advancing the understanding of stem cell dynamics, tissue regeneration, and the molecular cues that govern stem cell niche interactions.
Peptide-Based Drug Discovery: The unique cyclic structure and high receptor selectivity of Balixafortide render it a valuable reference molecule in the design and evaluation of novel peptide-based CXCR4 inhibitors. Researchers utilize it as a benchmark for screening and optimizing new analogs, supporting structure-activity relationship studies and the development of next-generation peptide modulators. This application underscores its importance in the broader field of peptide chemistry and targeted molecular design, enabling the advancement of innovative research tools and chemical probes for CXCR4-related pathways.
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