VH 298 ( VH298;VH298 )

Catalog No. M13305 CAS No. 2097381-85-4

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Product Name

VH 298
Note

Research use only, not for human use.
Brief Description

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

A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays; 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; induces HIF transcriptional activity and upregulates HIF-dependent response gene products, elicits a HIF-dependent hypoxic response in various cell lines.
Synonyms

VH298;VH298
Pathway

PROTACs
Target

E3 Ligase Ligand
Recptor

E3 Ligase Ligand
Research Area

Metabolic Disease
Indication

——

CAS Number

2097381-85-4
Formula Weight

523.65
Molecular Formula

C27H33N5O4S
Purity

>98% (HPLC)
Solubility

——
SMILES

O=C([C@H]1N(C([C@@H](NC(C2(CC2)C#N)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3
Chemical Name

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

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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