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VH298
Axon 2810
CAS:
2097381-85-4
Purity:
98%
- Soluble in DMSO
- MF: C27H33N5O4S
- MW: 523.65
Description
VH298 is a potent and selective VHL inhibitor (Kd value of 80-90 nM) that stabilizes HIF-α and elicits a hypoxic response via the blockade of the VHL:HIF-α protein–protein interaction downstream of HIF-α hydroxylation by PHD enzymes.
More Information
| Parent CAS No. | 2097381-85-4 |
|---|---|
| Chemical Name | (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| MFCD | N.A. |
| Short Description | VHL inhibitor |
References
- J Frost et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat Commun. 2016 Nov 4;7:13312.
- P Soares 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. 2018 Jan 25;61(2):599-618.
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