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(S,R,S)-AHPC-C5-COOH
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(S,R,S)-AHPC-C5-COOH图片
CAS NO:2267282-19-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) 是一种合成的 E3 连接酶配体-连接蛋白偶联物,包含 VH032 配体和 linker。VH032 是强效选择性的针对 VHL/ HIF-1α 相互作用的抑制剂,Kd 值为的 185 nM,有潜力用于贫血和缺血性疾病的相关研究。
Cas No.2267282-19-7
别名VH032-C5-COOH
分子式C29H42N4O5S
分子量558.73
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

(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.