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Description

A 14-aa internally disulfide-bonded peptide that potently protects MT-4 cells against X4-HIV strain HIV-1IIIB infection (EC50 = 4 nM in 5 d, MOI = 0.01) by competing against SDF-1alpha/CXCL12 for CXCR4 binding (IC50 = 0.91 nM, [SDF-1] = 100 nM, CXCR4-expressing CHO cells), while exhibiting cytotoxicity only at much higher concentrations (CC50 = 56 µ,M, 5 d in MT-4 cultures by MTT assays). Shown to inhibit SDF-1-induced Ca2+ mobilization (IC50 = 4.5 nM, [SDF-1] = 30 nM, CXCR4-expressing CHO cells) and cell migration (1.01- and 1.41-fold of non-SDF-1-stimulated control, respectively, with or without 100 nM TF14016, [SDF-1] = 100 ng/mL, 5BC-5 cells) in cultures in vitro and effectively prevent CXCR4-dependent SCLC (small lung cancer cell) 5BC-5 metastasis in NK-depleted SCID mice in vivo (average # of lung foci/nodules 12 wks after 5BC-5 i.v. inoculation = 1.25 vs. 9.75, respectively, with or without daily 10 mg/kg i.p. dosage)., A 14-aa internally disulfide-bonded peptide that potently competes against SDF-1alpha/CXCL12 for CXCR4 binding (IC50 = 0.91 nM, [SDF-1] = 100 nM) and protects MT-4 cells against X4-HIV strain HIV-1IIIB infection (EC50 = 4 nM in 5 d, MOI = 0.01) with no significant cytotoxicity (CC50 = 56 µ,M, 5 d). Inhibits SDF-1-induced Ca2+ mobilization (IC50 = 4.5 nM, [SDF-1] = 30 nM, CXCR4-expressing CHO cells) in vitro and effectively prevents CXCR4-dependent 5BC-5 metastasis in NK-depleted SCID mice in vivo (10 mg/kg i.p.) in vivo.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.