CXCR4 Antagonist IV, TF14016

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-1_IIIB 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.

A 14-aa internally disulfide-bonded peptide that potently protects MT-4 cells against X4-HIV strain HIV-1_IIIB 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).

Cell permeable: yes

Primary Target
CXCR4

Toxicity: Standard Handling (A)

N^α-4-fluorobenzoyl-Arg-Arg-Nal-Cys⁴-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys¹³-Arg-NH₂ (Disulfide bond: 4 → 13; Nal = L-3-(2-naphthyl)alanine; Cit = L-citrulline)

Supplied as a trifluoroacetate salt.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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.

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