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Submit ReviewFluorescent HIF-1α peptide (Kd = 180-560 nM). 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.
λabs | 485 nm |
---|---|
λem | 520 nm |
Closest Laser line | 488 nm |
Application | Fluorescence polarization (FP) displacement assays |
M. Wt | 1477.48 |
Formula | C71H84N10O25 |
Sequence |
DEALAXYIPD (Modifications: Asp-1 = (5,6)-FAM-Asp, X-6 = Hyp) |
Storage | Store at -20°C |
Purity | ≥95% (HPLC) |
InChI Key | CWNCTVVEODBMBK-RHNKRQRVSA-N |
Smiles | O=C([C@@H]1CCCN1C([C@H]([C@@H](CC)C)NC([C@H](CC2=CC=C(O)C=C2)NC([C@@H]3C[C@@H](O)CN3C([C@@H](NC([C@H](CC(C)C)NC([C@@H](NC([C@H](CCC(O)=O)NC([C@@H](NC(C4=CC(C(O5)=O)=C(C=C4)C65C7=CC=C(O)C=C7OC8=C6C=CC(O)=C8)=O)CC(O)=O)=O)=O)C)=O)=O)C)=O)=O)=O)=O)N[C@@H](CC(O)=O)C(O)=O.O=C([C@@H]9CCCN9C([C@H]([C@@H](CC)C)NC([C@H](CC%10=CC=C(O)C=C%10)NC([C@@H]%11C[C@@H](O)CN%11C([C@@H](NC([C@H](CC(C)C)NC([C@@H](NC([C@H](CCC(O)=O)NC([C@@H](NC(C(C=C%12)=CC(C%13%14C%15=CC=C(O)C=C%15OC%16=C%13C=CC(O)=C%16)=C%12C(O%14)=O)=O)CC(O)=O)=O)=O)C)=O)=O)C)=O)=O)=O)=O)N[C@@H](CC(O)=O)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility | Soluble to 1 mg/ml in 0.01M PBS |
References are publications that support the biological activity of the product.
Buckley et al (2012) Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1a interaction J.Am.Chem.Soc. 134 4465 PMID: 22369643
Lucas et al (2018) Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase J.Med.Chem. 61 7387 PMID: 30040896
Roy et al (2019) SPR-measured kinetics of PROTAC ternary complexes influence target degradation rate. ACS Chem.Biol. 14 361 PMID: 30721025
Crew et al (2018) Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1 J.Med.Chem. 61 583 PMID: 28692295
Ahn et al (2009) HIF-1alpha peptide derivatives with modifications at the hydroxyproline residue as activators of HIF-1alpha Bioorg.Med.Chem.Lett. 19 4403 PMID: 19515556
If you know of a relevant reference for FAM-DEALA-Hyp-YIPD, please let us know.
Keywords: FAM-DEALA-Hyp-YIPD, FAM-DEALA-Hyp-YIPD supplier, Fluorescent, HIF-1α, peptides, Fluorescence, polarization, (FP), displacement, assays, hypoxia, inducible, factor, HIF, pathways, Other, Probes, Hypoxia, Inducible, Factors, Active, Degraders, 7287, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia