(S,R,S)-AHPC (VH032-NH2) TFA 是基于 VH032 的 VHL 配体，用于招募 von Hippel-Lindau (VHL) 蛋白。蛋白质降解剂 1 TFA 可以通过接头连接到蛋白质的配体（例如 BCR-ABL1）以形成 PROTAC（例如 GMB-475）。 GMB-475 在 Ba/F3 细胞中诱导 BCR-ABL1 降解，IC50 为 1.11 μM。
Protein degrader 1 TFA is a small molecule ligand for VHL, an E3 ligase which has been targeted in numerous PROTACs.
Synthesis of HaloPROTACs contains Protein degrader 1 (Degradation Inducing Moiety A). Protein degrader 1 (Degradation Inducing Moiety A) is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. HaloPROTACs containing Protein degrader 1 (Degradation Inducing Moiety A) lead to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used[1].
[1]. Buckley DL, et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.
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