Chemical Name: (2S,4R)-1-((2S)-2-(5-((5-((6-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)oxy)pentyl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Biological ActivityCRBN-6-5-5-VHL is a potent and selective cereblon Degrader (PROTAC®) (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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Application of CRBN-6-5-5-VHL in MM1S cells
Western blot data showing potent knockdown of Cereblon (CRBN) mediated by the Degrader: CRBN-6-5-5-VHL in MM1S cells after 16 h incubation. IKZF1 (Ikaros) and IKZF3 (Aiolos) are transcription factors and neosubstrates of Cereblon. Application of CRBN-6-5-5-VHL does not result in degradation of these proteins. Pom; Pomalidomide.
Data courtesy of Christian Steinebach, University of Bonn.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
PROTAC-mediated crosstalk between E3 ligases.
Steinebach et al.
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