TC 14012, Peptidomimetic CXCR4 antagonist (ab230364)

Overview

  • Product name

    TC 14012, Peptidomimetic CXCR4 antagonist
  • Description

    Peptidomimetic CXCR4 antagonist
  • Biological description

    TC 14012 is a peptidomimetic  CXCR4 antagonist. It blocks CXCR4-mediated HIV infection with an IC50 value of 19.3 nM. In addition, TC 14012 (100 μg/ml) inhibits CXCL12-induced phosphorylation of p42/44 MAPK and STAT3 in B cells from patients with chronic lymphocytic leukemia. TC 1412 is C-terminally amidated which results in high serum stability. TC 14012 is CXCR7 agonist (EC50 = 350 nM) promoting the recruitment of β-arrestin and Erk 1/2 phosphorylation.

  • Purity

    > 95%
  • CAS Number

    368874-34-4
  • Chemical structure

    Chemical Structure

Properties

  • Molecular weight

    2066.43
  • Molecular formula

    C90H140N34O19S2
  • Sequence

    RRACYXKXPYRXCR (Modifications: Disulfide bridge between 4-13, C-terminal amide, Ala-3 = 3-(2-naphthalenylalanine), X-6 and X-12 = L-Citrulline, X-8 = D-Citrulline)
  • PubChem identifier

    90488928
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • SMILES

    [H]N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC2=CC=CC=C2C=C1)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC1=O)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O
  • Source

    Synthetic

References

This product has been referenced in:

  • Dorsam RT & Gutkind JS G-protein-coupled receptors and cancer. Nat Rev Cancer 7:79-94 (2007). Read more (PubMed: 17251915) »
  • Tamamura H  et al. Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. J Med Chem 48:380-91 (2005). Read more (PubMed: 15658852) »
  • Broxmeyer HE  et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med 201:1307-18 (2005). Read more (PubMed: 15837815) »

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