ChemicalBook > CAS DataBase List > VH-032

VH-032

Product Name: VH-032
CAS No.: 1448188-62-2
Chemical Name: VH-032
Synonyms: VHL032;VH-032;N-Acetyl-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide;L-Prolinamide, N-acetyl-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;(2S,4R)-1-((S)-2-acetamido-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-[(2S)-2-acetamido-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide
CBNumber: CB54668649
Molecular Formula: C24H32N4O4S
Formula Weight: 472.6
MOL File: 1448188-62-2.mol

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VH-032 Property

Boiling point:: 778.5±60.0 °C(Predicted)
Density: 1.248±0.06 g/cm3(Predicted)
storage temp.: -20°C, sealed storage, away from moisture
solubility: DMSO: 200 mg/mL (423.19 mM)
pka: 14.07±0.40(Predicted)
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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VH-032 Chemical Properties,Usage,Production

Uses

VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs[1][2][3].

Biological Activity

VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

IC 50

VHL

References

[1]. Michael Zengerle, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7. [2]. Carles Galdeano, et al. 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 Oct 23;57(20):8657-63. [3]. Kwok-Ho Chan, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513.

VH-032 Preparation Products And Raw materials

Raw materials

Preparation Products

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1448188-62-2, VH-032Related Search:

VH-032

VHL032

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

L-Prolinamide, N-acetyl-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

(2S,4R)-1-[(2S)-2-acetamido-3,3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide

N-Acetyl-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide

1448188-62-2