(S,R,S)-AHPC (VH032-NH2) 是一种基于 VH032 的，可募集 von Hippel-Lindau (VHL) 蛋白的 VHL 配体。(S,R,S)-AHPC 可通过 linker 与靶蛋白配体 (比如 BCR-ABL1) 连接，形成 PROTAC 分子 (比如 GMB-475)。GMB-475 作用于 Ba/F3 细胞，诱导 BCR-ABL1 降解， IC50 为 1.11 μM。
货号:ajcx33416
CAS:1448297-52-6
分子式:C22H30N4O3S
分子量：430.56
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells[1].

The VHL protein is a substrate recognition subunit of two ubiquitously expressed and biologically important Cullin RING E3 ubiquitin ligase complexes. VHL is one of the most popular E3 ligases being recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and subsequent proteasomal degradation of a target protein.

[1]. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. Cancer Res. 2019 Jul 16. pii: canres.1236.2019.