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VH-298

Catalog No. TQ0121 CAS 2097381-85-4

VH-298 is a potent inhibitor of VHL 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.

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VH-298, CAS 2097381-85-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 229.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 622.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 100%

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Description	VH-298 is a potent inhibitor of VHL 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.
Targets&IC50	VHL/HIFα:80 to 90 nM (Kd)
In vitro	VH298, 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.?We show that 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.

Molecular Weight	523.65
Formula	C27H33N5O4S
CAS No.	2097381-85-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 78.3mg/ml (149.53 Mm)

References and Literature

1. Frost J, 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.

Citations

1. Wang J, Wen Y, Zhang Y, et al.An interpretable artificial intelligence framework for designing synthetic lethality-based anti-cancer combination therapies.Journal of Advanced Research.2023

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Angiogenesis related Compound Library Bioactive Compounds Library Max PPI Inhibitor Library Glutamine Metabolism Compound Library NO PAINS Compound Library Epigenetics Compound Library Bioactive Compound Library Glycometabolism Compound Library

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Keywords

VH-298 2097381-85-4 Angiogenesis Chromatin/Epigenetic Others PROTAC Ligand for E3 Ligase HIF E3 ligase-recruiting Moiety Inhibitor VH 298 Ligands for E3 Ligase inhibit VH298 inhibitor

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