| CAS | 1446322-66-2 |
| Sequence | H-Cys-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Pro-Gln-OH; cyclo(H-Cys-Leu-Leu-Phe-Val-Tyr-OH) (Disulfide bridge:Cys1-Cys1|) |
| Sequence Single | CGRKKRRQRRRPPQ; cyclo(CLLFVY) (Disulfide bridge:Cys1-Cys1|) |
| Molecular Formula | C111H188N42O24S2 |
| Molecular Weight | 2559.1 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | TAT-cyclo-CLLFVY is a selective HIF-1 heterodimerization inhibitor. TAT-cyclo-CLLFVY blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). TAT-cyclo-CLLFVY inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY also reduces tubularization of hypoxic HUVECs. |
| References | 1. A cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. Miranda et al (2013). J.Am.Chem.Soc. 135 10418 PMID: 23796364 |