TBK1 PROTAC® 3i
Chemical Name: (2S,4R)-1-((S)-18-(4-((5-Bromo-4-((3-(N-methylcyclobutanecarboxamido)propyl)amino)pyrimidin-2-yl)amino)phenoxy)-2-(tert-butyl)-4-oxo-6,10,15-trioxa-3-azaoctadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Biological ActivityTBK1 PROTAC® 3i is a potent TANK-binding kinase 1 (TBK1) PROTAC® Degrader (DC50 = 12 nM, Dmax = 96%). Exhibits >50-fold selectivity for TBK1 over the closely related IKKε. Comprises a ligand for von-Hippel Lindau (VHL) protein joined by a linker to a TBK1-targeting moiety. Brings about near complete degradation of TBK1 in mutant K-Ras and wild-type cancer cell lines with no significant effect of proliferation.
Negative control TBK1 control PROTAC® 4 (Cat. No. 7260) also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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.
Identification and characterization of Von Hippel-Lindau-recruiting proteolysis targeting chimeras (PROTACs) of TANK-binding kinase 1.
Crew et al.
Citation for TBK1 PROTAC® 3i
The citations listed below are publications that use Tocris products. Selected citations for TBK1 PROTAC® 3i include:
1 Citation: Showing 1 - 1
Targeting TBK1 to overcome resistance to cancer immunotherapy.
Authors: Sun Et al.
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