VH 298
Chemical Name: (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98%
Biological Activity
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.
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.Technical Data
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.
Additional Information
Background References
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Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition.
Frost et al.
Nat.Commun., 2016;7:13312 -
RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response.
Frost et al.
Wellcome Open Res., 2019;4:17 -
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.
Soares et al.
J.Med.Chem., 2018;61:599
Product Datasheets
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Citations for VH 298
The citations listed below are publications that use Tocris products. Selected citations for VH 298 include:
2 Citations: Showing 1 - 2
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Genome-Wide Interrogation of Human Cancers Identifies EGLN1 Dependency in Clear Cell Ovarian Cancers.
Authors: Price Et al.
Cancer Res 2019;79:2564
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Von Hippel-Lindau (VHL) Protein Antagonist VH298 Improves Wound Healing in Streptozotocin-Induced Hyperglycaemic Rats by Activating Hypoxia-Inducible Factor- (HIF-) 1 Signalling.
Authors: Qiu Et al.
J Diabetes Res 2019;2019:1897174
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