E3 ligase Ligand 1 |
| رقم الكتالوجGC32711 |
E3 ligase Ligand 1 (VHL ligand 2 hydrochloride) هو (S ، R ، S) - Ligand القائم على AHPC المستخدم في توظيف بروتين von Hippel-Lindau (VHL). يمكن استخدام E3 ligase Ligand 1 لتصنيع ARV-771 ، وهو مزيل مواد BET PROTAC يعتمد على ligase من von Hippel-Landau (VHL). يحلل ARV-771 بروتين BET بشكل فعال في خلايا سرطان البروستاتا المقاومة للإخصاء (CRPC) مع DC50 <1 نانومتر.
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Cas No.: 1948273-03-7
Sample solution is provided at 25 µL, 10mM.
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E3 ligase Ligand 1 is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.
E3 ligase Ligand 1 is a VHL E3 ligase-binding ligand[1]. E3 ligase Ligand 1 is used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC. ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition[2].
[1]. WO/2017/030814A1 [2]. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(26), 7124-7129
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