(S,R,S)-AHPC-C5-COOH (Synonyms: VH032-C5-COOH) |
| Catalog No.GC65133 |
(S,R,S)-AHPC-C5-COOH(VH032-C5-COOH)는 합성된 E3 리가제 리간드-링커 접합체이며 VH032 VHL 기반 리간드와 PROTAC를 형성하는 링커를 포함합니다. VH-032는 185nM의 Kd를 갖는 VHL/HIF-1α 상호작용의 선택적이고 강력한 억제제이며, 빈혈 및 허혈성 질환 연구에 대한 잠재력이 있습니다.
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Cas No.: 2267282-19-7
Sample solution is provided at 25 µL, 10mM.
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(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].
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.
[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.
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