Product Information
Applications
Biological Information
Primary TargetCXCR4
Primary Target IC<sub>50</sub>0.9 nM
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Peptide SequenceNα-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)
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

CXCR4 Antagonist IV, TF14016 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
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.

Revision31-May-2013 JSW
SynonymsFusin Antagonist IV
DescriptionA 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).
FormWhite solid
FormulationSupplied as a trifluoroacetate salt.
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
Peptide SequenceNα-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)
Purity≥95% by HPLC
SolubilityH₂O (100 mg/ml)
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesOtani, 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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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > G-Protein and Related