Overview

  • Product name

    VH298, VHL inhibitor
  • Description

    Potent, cell permeable VHL inhibitor
  • Biological description

    VH298 is a cell permeable compound that binds tightly to VHL (KD = 80- 90 nM in in vitro binding assays) leading to cellular accumulation of HIF1-α. VH298 selectively stabilizes hydroxylated HIF1-α and induces HIF-dependent transcription.

  • Purity

    > 98%
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (2S,4R)-1-[(2S)-2-[(1-cyanocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide

  • Molecular weight

    523.65
  • Molecular formula

    C27H33N5O4S
  • PubChem identifier

    122199236
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    100 mM in DMSO

    100mM in ethanol

  • SMILES

    CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)C4(CC4)C#N)O
  • Source

    Synthetic

References

This product has been referenced in:

  • Soares P  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)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298). J Med Chem 61:599-618 (2018). Read more (PubMed: 28853884) »
  • Frost J  et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-a hydroxylation via VHL inhibition. Nat Commun 7:13312 (2016). Read more (PubMed: 27811928) »

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