VH 032 New
Chemical Name: (2S,4R)-1-((S)-2-Acetamido-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Biological ActivityVH 032 is an inhibitor of E3 ubiquitin ligase VHL (Kd = 185 nM). Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. VH 032 treatment causes dose dependent upregulation of HIF-target genes including CA9, GLUT1 and PHD2 in different cell lines. Cell permeable.
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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.
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