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| | TC 14012 (trifluoroacetate salt) Basic information |
| | TC 14012 (trifluoroacetate salt) Chemical Properties |
| solubility | DMSO: 10 mg/mlPBS (pH 7.2): 10 mg/ml |
| | TC 14012 (trifluoroacetate salt) Usage And Synthesis |
| Description | 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. TC 14012 is an antagonist of CXCR4, blocking 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. This peptidomimetic is C-terminally amidated, resulting in high stability in serum. TC 14012 also activates CXCR7 (EC50 = 350 nM), resulting in the recruitment of β-arrestin and Erk ½ phosphorylation. | | References | [1] HIROKAZU TAMAMURA. T140 analogs as CXCR4 antagonists identified as anti-metastatic agents in the treatment of breast cancer[J]. FEBS Letters, 2003, 550 1-3: 79-83. DOI: 10.1016/s0014-5793(03)00824-x
[2] STéPHANIE GRAVEL. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains.[J]. The Journal of Biological Chemistry, 2010: 37939-37943. DOI: 10.1074/jbc.c110.147470
[3] HIROKAZU TAMAMURA . Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140[J]. Bioorganic & Medicinal Chemistry Letters, 2001, 11 14: Pages 1897-1902. DOI: 10.1016/s0960-894x(01)00323-7
[4] SHENG ZHANG . Activation of CXCR7 alleviates cardiac insufficiency after myocardial infarction by promoting angiogenesis and reducing apoptosis[J]. Biomedicine & Pharmacotherapy, 2020, 127: Article 110168. DOI: 10.1016/j.biopha.2020.110168 |
| | TC 14012 (trifluoroacetate salt) Preparation Products And Raw materials |
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