CRBN-6-5-5-VHL 是一种有效且选择性的基于 von Hippel-Lindau 的 cereblon (CRBN) 降解剂,DC50 值为 1.5 nM。 CRBN-6-5-5-VHL对新底物IKZF1和IKZF3的降解几乎没有影响。
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Potent and selective cereblon degrader (DC50 = 1.5 nM). Induces complete degradation of cereblon in MM1S cells. Comprises a cereblon E3 ligase ligand joined by a linker to a ligand for the E3 ligase VHL. Cell-permeable.
Steinebach et al (2019) PROTAC-mediated crosstalk between E3 ligases. Chem.Commun.(Camb) 55 1821 PMID:30672516
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