Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.
CAT No: HB00088
CAS No:664334-36-5
Synonyms/Alias:Motixafortide;BKT140;664334-36-5;BKT140 acetate salt;Motixafortide (BL-8040);GLXC-20012;s9665;AKOS032944983;AS-84209;DA-61745;F85502;Bz(4-F)-Arg-Arg-2Nal-Cys(1)-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys(1)-Arg-NH2;N2-(4-Fluorobenzoyl)-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-DLys-Pro-Tyr-Arg-Cit-Cys-Arg-NH2;
BKT140, also known as 4F-benzoyl-TN14003 or TN14003 analog, is a synthetic peptide derivative designed to interact specifically with chemokine receptors, particularly CXCR4. This compound has garnered significant attention in scientific research due to its high affinity and selectivity for CXCR4, a receptor implicated in various biological processes. BKT140 features a modified peptide backbone that enhances its stability and bioactivity, making it a valuable tool for probing receptor-ligand interactions in vitro and in vivo. Its robust binding characteristics and resistance to enzymatic degradation set it apart from earlier peptide analogs, enabling more precise studies in cellular signaling and molecular biology. The unique properties of BKT140 facilitate its use in diverse experimental settings, supporting advanced research in cellular migration, immune response modulation, and beyond.
Cancer Metastasis Research: In oncology research, BKT140 is extensively utilized to investigate the mechanisms underlying tumor cell migration and metastasis. By selectively targeting the CXCR4 receptor, this peptide analog allows researchers to dissect the signaling pathways that drive cancer cell invasion and dissemination. Its application in in vitro migration assays and animal models has provided critical insights into the role of CXCR4 in facilitating the spread of malignant cells, particularly in breast, prostate, and hematological cancers. The ability to modulate receptor activity with BKT140 supports the identification of novel therapeutic targets and the development of anti-metastatic strategies, advancing the understanding of tumor biology at the molecular level.
Stem Cell Mobilization Studies: BKT140 is a powerful tool for studying stem cell trafficking, especially in the context of hematopoietic stem cell mobilization. CXCR4 plays a pivotal role in retaining stem cells within the bone marrow niche, and the application of this compound enables researchers to investigate the mechanisms that govern stem cell egress. By antagonizing CXCR4, BKT140 facilitates the release of stem cells into the peripheral circulation, providing a model to study stem cell dynamics and homing processes. These insights are instrumental for optimizing protocols in regenerative medicine and transplantation research, where efficient mobilization and engraftment of stem cells are critical for therapeutic success.
HIV Entry Inhibition Research: The CXCR4 receptor is a key co-receptor for HIV-1 entry into host cells, making it a target of interest in virology research. BKT140 has demonstrated utility in blocking the interaction between the viral envelope glycoprotein and CXCR4, thereby inhibiting viral entry and replication in vitro. Its application in cellular assays has helped clarify the molecular determinants of HIV tropism and the role of chemokine receptors in viral pathogenesis. By providing a selective means to disrupt HIV-host cell interactions, this peptide analog supports the evaluation of novel antiviral strategies and the exploration of chemokine receptor biology in infectious disease models.
Leukocyte Trafficking and Inflammation: In immunology, BKT140 is employed to elucidate the mechanisms of leukocyte migration during inflammatory responses. By interfering with CXCR4-mediated signaling, it allows researchers to assess how immune cells are recruited to sites of injury or infection. Experimental models utilizing this compound have shed light on the regulation of immune cell positioning, activation, and function. These studies contribute to a deeper understanding of inflammatory diseases and immune system homeostasis, informing the development of targeted interventions for conditions characterized by aberrant leukocyte trafficking.
Drug Discovery and Receptor Pharmacology: The specificity and potency of BKT140 make it an ideal candidate for high-throughput screening assays in drug discovery. Researchers employ it as a reference compound to benchmark the activity of new CXCR4 modulators or to validate assay systems designed to measure receptor-ligand interactions. Its well-characterized pharmacological profile aids in dissecting the structure-activity relationships of chemokine receptor antagonists, facilitating the identification and optimization of novel therapeutic leads. In addition, BKT140 serves as a valuable control in studies exploring the broader physiological roles of CXCR4 in development, immune surveillance, and tissue repair, further expanding its utility across diverse research disciplines.
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