UNC 6852 is a polycomb repressive complex 2 (PRC2) Degrader (PROTAC™; DC50 = 0.79 μM). It comprises an EED (embryonic ectoderm development) based ligand, joined by a linker to a von Hippel-Lindau ligand. In B lymphoblast cell lines, UNC 6852 selectively degrades PRC2 components EED (DC50 = 0.31 μM, Dmax = 94%), enhancer of zeste homolog 2 (EZH2, DC50 = 0.67 μM, Dmax = 96%), and suppressor of zeste homolog 12 (SUZ12, DC50 = 0.59 μM, Dmax = 82%). In zebrafish, UNC 6852 treatment increases transcription of
tfpia
and prolongs time to occlusion (TTO) in the caudal vein following laser injury.
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-124611 |
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| Réf. fabricant | 18795805 |
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| Nom chimique ou matériau | (2 S,4 R)-1-(-2-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4 ]triazolo[4,3-c]pyrimidin-8-yl)benzamido)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
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| CAS | 2688842-08-0 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>43</sub>H<sub>48</sub>N<sub>10</sub>O<sub>6</sub>S |
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| Pureté | 0.98 |
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