| 货号 | 11974-10mg |
| 描述 | C-X-C chemokine receptor type 4 (CXCR4) is a receptor for the stromal cell-derived factor-1 which is designated as chemokine ligand 12 (CXCL12). It is involved in cell progression, hematopoiesis, cancer, HIV entry, and rheumatoid arthritis.1,2,3 TC 14012 is an antagonist of CXCR4, blocking CXCR4-mediated HIV infection with an IC50 value of 19.3 nM.4 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.5 This peptidomimetic is C-terminally amidated, resulting in high stability in serum.4 TC 14012 also activates CXCR7 (EC50 = 350 nM), resulting in the recruitment of β-arrestin and Erk ½ phosphorylation.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Broxmeyer, H.E.,Orschell, C.M.,Clapp, D.W., et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. Journal of Experimental Medicine 201(8), 1307-1318 (2005). 2.Dorsam, R.T., and Gutkind, J.S. G-protein-coupled receptors and cancer. Nature Reviews.Cancer 7, 79-94 (2007). 3.Tamamura, H.,Hiramatsu, K.,Ueda, S., 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. Journal of Medicinal Chemistry 48, 380-391 (2005). 4.Tamamura, H.,Omagari, A.,Hiramatsu, K., 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. Bioorganic & Medicinal Chemistry Letters 11(14), 1897-1902 (2001). 5.Burger, M.,Hartmann, T.,Krome, M., et al. Small peptide inhibitors of the CXCR4 chemokine receptor (CD184) antagonize the activation, migration, and antiapoptotic responses of CXCL12 in chronic lymphocytic leukemia B cells. Blood 106(5), 1824-1830 (2005). 6.Gravel, S.,Malouf, C.,Boulais, P.E., et al. The peptidomimetic CXCR4 antagonist TC14012 recruits β-arrestin to CXCR7: Roles of receptor domains. The Journal of Biological Chemisty 285(49), 37939-37943 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 2066.4 |
| 分子式 | C90H140N34O19S2 |
| CAS号 | 368874-34-4 |
| 稳定性 | ≥ 2 years |
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