BL-8040

BL-8040 화학적 특성, 용도, 생산

• 효소 저해제

  This orally bioavailable, disulfide cross-linked, polyphemusin-II-derived peptide antagonist (sequence shown above, with Nal = naphthylamine, Cit = citrulline, D-Lys = D-Lysine, and Cys = half-cystine), also known as 4-Fbenzoyl-TN14003 and BL-8040, targets CXC Chemokine Receptor-4 (CXCR4), a G-protein-coupled receptor that is directly involved in tumor progression, tumor angiogenesis, metastasis, and cancer cell survival. Primary Mode of Inhibitory Action: CXCR4 is over-expressed in more than 70% of human cancers and its expression often correlates with disease severity. BKT140 exhibits high affinity (Ki = 0.8nM) and a low rate of dissociation from its receptor. BKT140 prevents the binding of stromal derived factor-1 (SDF-1 or CXCL12) to CXCR4 activation, resulting in decreased tumor cell proliferation and migration. In addition, inhibition of CXCR4 may mobilize hematopoietic cell egress from the bone marrow and into blood. BKT140 significantly and preferentially stimulates multiple myeloma apoptotic cell death, as indicated by induced morphological changes, phosphatidylserine externalization, decreased mitochondrial membrane potential, caspase-3 activation, sub-G1 cell-cycle arrest, as well as DNA double-stranded breaks.

BL-8040 공급 업체

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