VH298

Based on 2 reference(s) in Google Scholar 8 10 2

Axon 2810

CAS [2097381-85-4]

MF C27H33N5O4S
MW 523.65

Purity: 98%
Soluble in DMSO

VH298

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.

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.

Inhibitor of E3 ubiquitin-protein ligase VHL

Chemical name

(2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Parent CAS No.

[2097381-85-4]

产品资料