| Sequence | (5,6)-FAM-Asp-Glu-Ala-Leu-Ala-Hyp-Tyr-Ile-Pro-Asp-OH |
| Sequence Single | (5,6)-FAM-Asp-EALA-Hyp-YIPD |
| Molecular Formula | C71H84N10O25 |
| Molecular Weight | 1477.48 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | FAM-DEALA-Hyp-YIPD is a fluorescent HIF-1α peptide (Kd = 180-560 nM). FAM-DEALA-Hyp-YIPD can be used to assess VHL binding in Fluorescence Polarization (FP) displacement assay, and evaluate the effect of VHL binding on degradation activity. Excitation maximum = 485 nm, emission maximum = 535 nm. Longer peptide version, FAM-DEALAHypYIPMDDDFQLRSF, also available. |
| References | 1. Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1a interaction. Buckley et al (2012). J.Am.Chem.Soc. 134 4465 PMID: 22369643 2. Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase. Lucas et al (2018). J.Med.Chem. 61 7387 PMID: 30040896 3. SPR-measured kinetics of PROTAC ternary complexes influence target degradation rate. Roy et al (2019). ACS Chem.Biol. 14 361 PMID: 30721025 4. Identification and characterization of von Hippel-Lindau-recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-binding kinase 1. Crews et al (2018). J.Med.Chem. 61 583 PMID: 28692295 5. HIF-1α peptide derivatives with modifications at the hydroxyproline residue as activators of HIF-1α. Ahn et al (2009). Bioorg.Med.Chem.Lett. 19 4403 PMID: 19515556 |