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Description
Overview
A 14-aa internally disulfide-bonded peptide that potently competes against SDF-1α/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 µM; 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.
Catalogue Number
500507
Brand Family
Calbiochem®
Synonyms
Fusin Antagonist IV
References
References
Otani, Y., et al. 2012. FEBS Lett.586, 3639. Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem.10, 5720. Tamamura, H., et al. 2003. Org. Biomol. Chem.1 3663. Tamamura, H., et al. 2003. Org. Biomol. Chem.1, 3656.
Otani, Y., et al. 2012. FEBS Lett.586, 3639. Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem.10, 5720. Tamamura, H., et al. 2003. Org. Biomol. Chem.1 3663. Tamamura, H., et al. 2003. Org. Biomol. Chem.1, 3656.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
31-May-2013 JSW
Synonyms
Fusin Antagonist IV
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-1α/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 µM; 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).
