(S,R,S)-AHPC-Me dihydrochloride (Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride) |
| カタログ番号GC60426 |
(S,R,S)-AHPC-Me 二塩酸塩 (VHL リガンド 2 二塩酸塩) は、von Hippel-Lindau (VHL) タンパク質の動員に使用される (S,R,S)-AHPC ベースの VHL リガンドです。 (S,R,S)-AHPC-Me 二塩酸塩は、フォン ヒッペル-ランダウ (VHL) E3 リガーゼベースの BET PROTAC 分解剤である ARV-771 の合成に使用できます。 ARV-771 は、去勢抵抗性前立腺癌 (CRPC) 細胞の BET タンパク質を DC50 <1 nM で強力に分解します。
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Sample solution is provided at 25 µL, 10mM.
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(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein[1]. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM[2].
[1]. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.
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