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VH298

Chemical Structure : VH298

CAS No.: 2097381-85-4

VH298 (VH-298;VH298)

Catalog No.: PC-61056Not For Human Use, Lab Use Only.

VH 298 is a potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

VH 298 is a potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.
VH 298 selectively engages VHL as its prime cellular target and is not toxic to cells, induces concentration- and time-dependent on-target specific accumulation of hydroxylated HIF-α in human cell lines.
VH 298 induces HIF transcriptional activity and upregulates HIF-dependent response gene products, elicits a HIF-dependent hypoxic response in various cell lines.

Physicochemical Properties

M.Wt 523.652
Formula C27H33N5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Soares P, et al. J Med Chem. 2017 Sep 18. doi: 10.1021/acs.jmedchem.7b00675.

2. Frost J, et al. Nat Commun. 2016 Nov 4;7:13312.

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