VH 032, amine hydrochloride

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Cat.No. 6462 - VH 032, amine hydrochloride | C22H30N4O3S.HCl | CAS No. 1448189-80-7
Description: Functionalized VHL ligand for PROTACs
Chemical Name: (4R)-3-Methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Derivative of the von Hippel-Lindau (VHL) ligand, VH 032, commonly used as a precursor to PROTACs that hijack VHL as the E3 ubiquitin ligase component. Supplied with a primary amine functional handle at a position known not to significantly affect binding to VHL, for ready conjugation to a linker/target protein ligand.

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Technical Data

M. Wt 467.02
Formula C22H30N4O3S.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1448189-80-7
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)N)=O)O)=O)SC=N1.Cl

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 46.7 100
DMSO 46.7 100

Preparing Stock Solutions

The following data is based on the product molecular weight 467.02. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.14 mL 10.71 mL 21.41 mL
5 mM 0.43 mL 2.14 mL 4.28 mL
10 mM 0.21 mL 1.07 mL 2.14 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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References

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

Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS Chem.Biol. 10 1770 PMID: 26035625

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


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