Description
TC 14012 is a peptidomimetic antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 2.9 nM) and CXCR7 agonist.1,2 It induces β-arrestin recruitment in HEK293T cells expressing CXCR7 (EC50 = 350 nM).1 TC 14012 reduces the cytopathic effect of HIV in infected MT-4 cells (EC50 = 0.4 nM) and inhibits HIV entry in vitro in a CXCR4-dependent manner (IC50 = 19.3 nM).3 It inhibits migration induced by chemokine (C-X-C motif) ligand 12 (CXCL12) in MDA-MB-231 breast cancer cells and human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 10 to 1,000 nM.2 TC 14012 (10 mg/kg) decreases infarct size in a mouse model of acute myocardial infarction induced by left anterior descending (LAD) coronary artery ligation.4WARNING This product is not for human or veterinary use.
References
[1] 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
[2] 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
[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
