(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate , contains the VH032 VHL-based ligand and a linker to form PROTAC s. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a K d of 185 nM, has the potential for the study of anemia and ischemic diseases
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.The von Hippel–Lindau tumor suppressor protein is the substrate-binding subunit of the VHL E3 ubiquitin ligase, it targets hydroxylated α subunit of HIFs for ubiquitination and subsequent proteasomal degradation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.