(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。
| 生物活性 |
(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. |
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| 体外研究 |
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. |
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| 分子式 |
C22H30N4O3S
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| 分子量 |
430.56
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| CAS号 |
1448297-52-6
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 科研文献 |
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