VH 032

Name: VH 032
Brand: Tocris Bioscience
SKU: 7774

Tocris Bioscience, part of Bio-Techne | Catalog # 7774

COA / SDS

Inhibitor of VHL; blocks interaction of VHL and HIF-α

Key Product Details

Description:	Inhibitor of VHL; blocks interaction of VHL and HIF-α
Chemical Name:	(2S,4R)-1-((S)-2-Acetamido-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	472.6

View Full Technical Details for VH 032

Technical Data
Citations

Biological Activity for VH 032

VH 032 is an inhibitor of E3 ubiquitin ligase VHL (K_d = 185 nM). Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. VH 032 treatment causes dose dependent upregulation of HIF-target genes including CA9, GLUT1 and PHD2 in different cell lines. Cell permeable.

Technical Data for VH 032

M. Wt	472.6
Formula	C₂₄H₃₂N₄O₄S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1448188-62-2
PubChem ID	77232228
InChi Key	GFVIEZBZIUKYOG-SVFBPWRDSA-N
Smiles	CC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for VH 032

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	47.26	100
	ethanol	47.26	100

Preparing Stock Solutions for VH 032

The following data is based on the product molecular weight 472.6.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.12 mL	10.58 mL	21.16 mL
5 mM	0.42 mL	2.12 mL	4.23 mL
10 mM	0.21 mL	1.06 mL	2.12 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

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References for VH 032

References are publications that support the biological activity of the product.

Frost Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 2016 PMID: 27811928
Galdeano Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von Hippel-Lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities. J.Med.Chem. 2014 PMID: 25166285