| Bioactivity | TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity[1][2]. |
| Invitro | TC14012 TFA (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 TFA (1 mM) does not inhibit all the infection of the CCR5-expressing cells by the SF162 (R5) or 89.6 (dualtropic) strain[1]. TC14012 TFA leads to erk 1/2 phosphorylation in U373 cells, which express endogenous CXCR7 but not CXCR4. Upon stimulation with TC14012 TFA, CXCR7 and the CXCR7-Cter4 chimera are able to recruit arrestin, whereas CXCR4 and CXCR4-Cter7 remain silent[2]. |
| Name | TC14012 TFA |
| Shortening | RR-{2Nal}-CY-{Cit}-K-{Cit}-PYR-{Cit}-CR-NH2 (Disulfide bridge:Cys4-Cys13) |
| Formula | C92H141F3N34O21S2 |
| Molar Mass | 2180.44 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |