VH 298

Key Product Details

Product Description

VH 298 is a high-affinity inhibitor of E3 ubiquitin ligase VHL (K_d = 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.

Licensing Information

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.

Product Specifications for VH 298

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.91 mL	9.55 mL	19.10 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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 9 publications citing the usage of this product.

• Soares 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. 2018 PMID: 28853884
• Frost RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response. Wellcome Open Res. 2019 PMID: 30801039
• Frost Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 2015 PMID: 27811928

Product Documents for VH 298