HaloPROTAC 2 (HaloPROTAC 2) 是 E3 和 21 原子长度接头的配体缀合物。接头的接头是卤素基团。 HaloPROTAC 2 包含基于 VH032 的 VHL 配体和 5 单元 PEG 接头。 HaloPROTAC 2 能够在基于细胞的测定中诱导 GFP-HaloTag7 的降解。
HaloPROTAC 2, a chloroalkane-containing PROTAC, induces degradation of HaloTag fusion proteins.
HaloPROTAC 1 and HaloPROTAC2, containing different linker lengths, are synthesized. Their ability to degrade GFP-HaloTag7, (stably expressed in HEK 293 cells) is tested tby flow cytometry, measuring changes in mean fluorescence intensity. While 24 hour treatment with HaloPROTAC 1 leads to less than 20% degradation, the longer HaloPROTAC2 leads to nearly 70% degradation of GFP-Halotag7 at 2.5 μM[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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