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Biological Activity for VH 298
VH 298 is a 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, with similar transcriptional profile to hypoxia. Cell permeable.
Negative control cis VH 298 also available.
Sold under licence from the University of Dundee
External Portal Information for VH 298
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.
Compound Libraries for VH 298
Technical Data for VH 298
|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.
Solubility Data for VH 298
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for VH 298
The following data is based on the product molecular weight 523.65. Batch specific molecular weights may vary from batch to batch due to the degree 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 for VH 298
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
Frost et al (2019) RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response. Wellcome Open Res. 4 17 PMID: 30801039
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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, 6156, Tocris Bioscience
2 Citations for VH 298
Citations are publications that use Tocris products. Selected citations for VH 298 include:
Price et al (2019) Genome-Wide Interrogation of Human Cancers Identifies EGLN1 Dependency in Clear Cell Ovarian Cancers. Cancer Res 79 2564 PMID: 30898838
Qiu et al (2019) Von Hippel-Lindau (VHL) Protein Antagonist VH298 Improves Wound Healing in Streptozotocin-Induced Hyperglycaemic Rats by Activating Hypoxia-Inducible Factor- (HIF-) 1 Signalling. J Diabetes Res 2019 1897174 PMID: 30911550
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