(S,R,S)-AHPC hydrochloride 是基于 VH032 的 VHL 配体,可用于募集 von Hippel-Lindau (VHL) 蛋白。它能够利用 linker 与靶蛋白配体连接,得到 PROTAC 分子。
产品描述
Protein degrader 1 hydrochloride is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).
体外活性
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes.Protein degraders have the power to abrogate all of the functions of a drug target at once, including scaffolding functions which are difficult to target with small molecule inhibitors. A novel class of PROTACs that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins is developed. HaloPROTACs will inspire the development of future PROTACs with more drug-like properties. In HEK 293 cellsstably expressing GFP-HaloTag7,24 hour treatment with HaloPROTAC1 leads to less than 20% degradation, the longer HaloPROTAC2 leads to nearly 70% degradation of GFP-Halotag7 at 2.5 μM.HaloPROTACs containing protein degrader 1 leads to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used
Cas No.
1448189-80-7
分子式
C22H31ClN4O3S
分子量
467.03
别名
Protein degrader 1 hydrochloride;ULM-1;VHL Ligand 1 hydrochloride
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years