VH-298

- Overview
  - Description: VH-298 is a novel and highly potent inhibitor of the VHL:HIF-α protein-protein interaction with a Kd value of 80 to 90 nM, and has been used in PROTAC technology. Chemical strategies to using small molecules to stimulate hypoxia inducible factors (HIFs) activity and trigger a hypoxic response under normoxic conditions, such as iron chelators and inhibitors of prolyl hydroxylase domain (PHD) enzymes, have broad-spectrum activities and off-target effects. VH298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes. VH298 engages with high affinity and specificity with VHL as its only major cellular target, leading to selective on-target accumulation of hydroxylated HIF-α in a concentration- and time-dependent fashion in different cell lines, with subsequent upregulation of HIF-target genes at both mRNA and protein levels. VH298 represents a high-quality chemical probe of the HIF signalling cascade and an attractive starting point to the development of potential new therapeutics targeting hypoxia signalling.
    
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- Properties
  - Categories
    
    Ligands for E3 Ligase
    
    CAS Number
    
    2097381-85-4
    
    Molecular Formula
    
    C27H33N5O4S
    
    Molecular Weight
    
    523.65
    
    Purity
    
    ≥98%
    
    Storage
    
    Powder: store in -20°C freezer for up to three years, store in 4°C freezer for up to two years
    In solvent: store in -80°C freezer for up to six months, store in -20°C freezer for up to two months
    
    Shipping
    
    Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
    
    SMILES
    
    O=C([ C@H
    
    * For research use only

VH-298

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