TC14012

CAS No. 368874-34-4

TC14012 ( —— )

Catalog No. M23116 CAS No. 368874-34-4

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TC14012
  • Note
    Research use only, not for human use.
  • Brief Description
    TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity.
  • Description
    TC14012 (1 mM) inhibits more than 95% the infection of the CXCR4-expressing cells by the HXB2 (X4) or 89.6 (dual-tropic) strain whereas TC14012 (1 mM) does not inhibit all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain.TC14012 leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4. Upon stimulation with TC14012, CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin, whereas CXCR4 and CXCR4-Cter7 remain silent.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Autophagy
  • Target
    CXCR
  • Recptor
    CXCR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    368874-34-4
  • Formula Weight
    2066.42
  • Molecular Formula
    C??H???N??O??S?
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 25 mg/mL (12.10 mM; Need ultrasonic)
  • SMILES
    ——
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. H Tamamura, et al. Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902. 2. Stéphanie Gravel, et al. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem. 2010 Dec 3;285(49):37939-43.
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