| Identification | Back Directory | [Name]
VH-032 | [CAS]
1448188-62-2 | [Synonyms]
VH-032
VHL032
(2S,4R)-1-((S)-2-acetamido-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide | [Molecular Formula]
C24H32N4O4S | [MDL Number]
MFCD33548811 | [MOL File]
1448188-62-2.mol | [Molecular Weight]
472.6 |
| Chemical Properties | Back Directory | [Boiling point ]
778.5±60.0 °C(Predicted) | [density ]
1.248±0.06 g/cm3(Predicted) | [solubility ]
DMSO: 200 mg/mL (423.19 mM) | [form ]
Solid | [pka]
14.07±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. |
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