XY-06-007 is a highly selective and potent Bump and Hole TAG Degrader (DC50,6h = 10 nM, T1/2 < 43.2 min). XY-06-007 comprises a cereblon (CRBN) E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (thebump bearer) that selectively binds the Brd4BD1 L94V variant (thehole). In cell lines expressing a fusion of the target protein with the tag, Brd4BD1 L94V, XY-06-007 drives formation of a ternary complex between CRBN and the tagged protein, leading to ubiquitination and subsequent proteasomal degradation of the entire protein. XY-06-007 is highly selective for Brd4BD1 L94V over wild-type, and is broadly selective across the proteome. XY-06-007 can be combined with the dTAG approach to achieve simultaneous degrader-mediated depletion of their respective protein fusions. XY-06-007 is suitable for
in vivo
studies.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-125071 |
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| Réf. fabricant | 18034022 |
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| Nom chimique ou matériau | (2R)-2-((S)-6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-(5-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)pentyl)propanamide |
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| CAS | 2757045-94-4 |
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| Quantité | 5 mg |
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| Cible | TAG Degradation Platforms |
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| Formule moléculaire | C<sub>41</sub>H<sub>41</sub>ClN<sub>8</sub>O<sub>8</sub> |
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| Pureté | 98% |
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