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.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-158133 |
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| Réf. fabricant | 18054992 |
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| Nom chimique ou matériau | (2 S,4 R)-1-(-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 |
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| CAS | 2052306-13-3 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>53</sub>H<sub>74</sub>BrN<sub>9</sub>O<sub>9</sub>S |
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| Pureté | 0.98 |
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