(S,R,S)-AHPC-C5-COOH

Names

[ Name ]:
(S,R,S)-AHPC-C5-COOH

Biological Activity

[Description]:

(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 PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

Signaling Pathways >> PROTAC >> E3 Ligase Ligand-Linker Conjugate

[Target]

VHL

[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.

[References]

[1]. Soares P, et al. Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).J Med Chem. 2018 Jan 25;61(2):599-618.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₄₂N₄O₅S

[ Molecular Weight ]:
558.73

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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