VH 032

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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)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity for VH 032

VH 032 is an inhibitor of E3 ubiquitin ligase VHL (Kd = 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 Data 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.

Select a batch to recalculate based on the batch molecular weight:
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.

Galdeano et al (2014) 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. 57 8657 PMID: 25166285

Frost et al (2016) Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat.Commun. 7 13312 PMID: 27811928


If you know of a relevant reference for VH 032, please let us know.

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View all Ubiquitin E3 Ligase Inhibitors

Keywords: VH 032, VH 032 supplier, VH032, Inhibitors, Inhibition, inhibits, VHL, HIF-alpha, HIF-a, HIF-α, von, Hippel-Lindau, protein, E3, ubiquitin, ligase, Hypoxia, Inducible, Factors, Ubiquitin, Ligases, 7774, Tocris Bioscience

Citations for VH 032

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