VH-032 free base · Synonyms: VH-032
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.
For research use only. Not for human or veterinary use.
Target
Ligands for E3 Ligase
Research area
Cancer
Purity >98%
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VH-032 structure
CAS No.: 1448188-62-2
Pack sizes & pricing
Description
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.
Biological activity
In Vitro 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
Identifiers
- SMILES
-
CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(C)=O)=O)=O)C=C2 - InChIKey
-
GFVIEZBZIUKYOG-SVFBPWRDSA-N
Specifications
- MW (average)
- 472.6000
- Formula
- C24H32N4O4S
- CAS No.
- 1448188-62-2
- Physical state
- Solid
- Color
- white to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, sealed storage, away from moisture; In solvent -20℃ 1 year.
Solubility
Soluble in DMSO
- In vitro
- DMSO:100 mg/mL
Documents
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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