BromoTag AGB1 is a highly selective and potent "Bump & Hole" TAG Degrader (DC50,6h < 15nM, T1/2 = 40 min). BromoTag AGB1 comprises a VHL E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4BD2 L387A variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4BD2 L387A, BromoTag AGB1 drives formation of a ternary complex between VHL and the "BromoTagged" protein, leading to ubiquitination of the protein and its subsequent proteasomal degradation. BromoTag AGB1 is highly selective for Brd4BD2 L387A over wild-type, and is broadly selective across the proteome. BromoTag AGB1 exhibits no cytoxicity in several cancer relevant cell lines. BromoTag AGB1 is suitable for
in vivo
studies.
Negative control BromoTag cis-AGB1 (Cat. No. 7687) also available.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125669 |
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| Réf. fabricant | 18737456 |
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| Nom chimique ou matériau | -13-((2 S,4 R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidine-1-carbonyl)-14,14-dimethyl-11-oxo-3,6,9-trioxa-12-azapentadecyl (R)-2-(-4-(4-chlorophenyl)-2,3,9-trimethyl-6 H-thieno[3,2-f][1,2,4 ]triazolo[4,3-a][1,4 ]diazepin-6-yl)butan |
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| Quantité | 5 mg |
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| Cible | TAG Degradation Platforms |
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| Formule moléculaire | C<sub>51</sub>H<sub>63</sub>ClN<sub>8</sub>O<sub>9</sub>S<sub>2</sub> |
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| Pureté | 98% |
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