Chemical Name: (2S,4R)-1-((S)-2-(1-cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Biological ActivityHigh-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition.
Frost et al.
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.
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
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
Genome-Wide Interrogation of Human Cancers Identifies EGLN1 Dependency in Clear Cell Ovarian Cancers.
Authors: Price Et al.
Cancer Res 2019;79:2564
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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