VH032是一种VHL配体，用于募集vonHippel-Lindau(VHL)蛋白。VH032是VHL/HIF-1α相互作用抑制剂，Kd为185nM。VH032可通过linker与靶蛋白配体连接，形成PROTAC分子。
货号:ajcx31802
CAS:1448188-62-2
分子式:C24H32N4O4S
分子量：472.6
溶解度:DMSO: 200 mg/mL (423.19 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

[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.