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TBK1 PROTAC® 3i

Catalog #: 7259
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TBK1 PROTAC® 3i | CAS No. 2052306-13-3 | Active Degraders
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Description: Potent TANK-binding kinase 1 (TBK1) PROTAC®

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

Purity: ≥98%

Product Details
Citations (1)
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Biological Activity

TBK1 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.

Technical Data

M.Wt:
1093.19
Formula:
C53H74BrN9O9S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2052306-13-3

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.

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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

  1. Targeting TBK1 to overcome resistance to cancer immunotherapy.
    Authors: Sun Et al.
    Nature  2023;615:158

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