High-affinity inhibitor of E3 ubiquitin ligase VHL (Kd = 80-90 nM). Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. Results in time- and concentration-dependent accumulation of hydroxylated HIF-α, and upregulates mRNA and protein levels of HIF target genes. Cell permeable. Negative control cis VH 298 also available.
Sold under licence from the University of Dundee
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of VH 298 is reviewed on the Chemical Probes website.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 523.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.91 mL||9.55 mL||19.1 mL|
|5 mM||0.38 mL||1.91 mL||3.82 mL|
|10 mM||0.19 mL||0.95 mL||1.91 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References are publications that support the biological activity of the product.
Frost et al (2015) Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 7 13312 PMID: 27811928
Soares et al (2018) Group-based optimization of potent and cell-active inhibitors of the von Hippel-Lindau (VHL) E3 ubiquitin ligase: structure-activity relationships leading to the chemical probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3 J.Med.Chem. 61 599 PMID: 28853884
If you know of a relevant reference for VH 298, please let us know.
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Keywords: VH 298, VH 298 supplier, Inhibitors, Inhibition, VH298, VHL, HIF-alpha, HIF-a, HIF-α, cisVH298, von, Hippel-Lindau, protein, E3, ubiquitin, ligase, Hypoxia, Inducible, Factors, Ubiquitin, Ligases, PROTACs, 6156, Tocris Bioscience
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