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Submit ReviewTBK1 PROTAC® 3i
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% (HPLC)
Biological Activity for TBK1 PROTAC® 3i
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) and TBK1 antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF9934 and NB100-56705.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for TBK1 PROTAC® 3i
| M. Wt | 1093.19 |
| Formula | C53H74BrN9O9S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2052306-13-3 |
| PubChem ID | 124108661 |
| InChI Key | QMGHHBHPDDAGGO-IIWOMYBWSA-N |
| Smiles | CN(C(C1CCC1)=O)CCCNC2=NC(NC3=CC=C(C=C3)OCCCOCCCCOCCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)O)=O)=O)=NC=C2Br |
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.
Solubility Data for TBK1 PROTAC® 3i
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 109.32 | 100 |
Preparing Stock Solutions for TBK1 PROTAC® 3i
The following data is based on the product molecular weight 1093.19. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.91 mL | 4.57 mL | 9.15 mL |
| 5 mM | 0.18 mL | 0.91 mL | 1.83 mL |
| 10 mM | 0.09 mL | 0.46 mL | 0.91 mL |
| 50 mM | 0.02 mL | 0.09 mL | 0.18 mL |
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Product Datasheets for TBK1 PROTAC® 3i
References for TBK1 PROTAC® 3i
References are publications that support the biological activity of the product.
Crew et al (2018) Identification and characterization of Von Hippel-Lindau-recruiting proteolysis targeting chimeras (PROTACs) of TANK-binding kinase 1. J.Med.Chem. 61 583 PMID: 28692295
If you know of a relevant reference for TBK1 PROTAC® 3i, please let us know.
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Keywords: TBK1 PROTAC® 3i, TBK1 PROTAC® 3i supplier, TANK-binding, kinase, 1, TBK1, potent, active, Degrader, Degraders, PROTACs, targeted, protein, degradation, TPD, von, Hippel, Lindau, VHL, E3, ligase, TANK, binding, (TBK), Kinase, 7259, Tocris Bioscience
1 Citation for TBK1 PROTAC® 3i
Citations are publications that use Tocris products. Selected citations for TBK1 PROTAC® 3i include:
Sun et al (2023) Targeting TBK1 to overcome resistance to cancer immunotherapy. Nature 615 158 PMID: 36634707
Do you know of a great paper that uses TBK1 PROTAC® 3i from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia