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

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Technical Data
Citations

Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

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

View all Ubiquitin Ligase (E3) Inhibitors »

Product Description

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.

Product Specifications

Molecular Weight

472.60

Formula

C₂₄H₃₂N₄O₄S

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

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

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.

Solubility

	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 472.60

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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

Calculators

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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Background References

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