| CAS | 368874-34-4 |
| Sequence | H-Arg-Arg-2-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2(Disulfide bridge between 4 - 13) |
| Sequence Single | RR-2-Nal-CY-Cit-K-D-Cit-PYR-Cit-CR-NH2 |
| Molecular Formula | C90H140N34O19S2 |
| Molecular Weight | 2066.43 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | TC 14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC 14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC 14012 has anti-HIV activity and anti-cancer activity. |
| References | 1. Synthesis of potent CXCR4 inhibitors possessing low cytotoxicity and improved biostability based on T140 derivatives. Tamamura et al (2003). Org.Biomol.Chem. 1 3656 PMID: 14649896 2. Small peptide inhibitors of the CXCR4 chemokine receptor (CS184) antagonize the activation, migration, and antiapoptotic responses of CXCL12 in chronic lymphocytic leukemia B cells. Burger et al (2005). Blood 106 1824 PMID: 15905192 3. The peptidomimetic CXCR4 antagonist TC14012 recruits beta arrestin to CXCR7: roles of receptor domains. Gravel et al (2010). J.Biol.Chem. 285 37939 PMID: 20956518 4. Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. H Tamamura, et al. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902. |