(+)-JQ1 based Degrader (PROTAC™) that selectively degrades BRD4
Cell penetrant Degrader (PROTAC®) compound based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. MZ 1 retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively). Exhibits potent cytotoxicity and antiproliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells).
Negative control cis MZ 1 also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-128553 |
| Réf. fabricant | 18749718 |
| Type de produit | Cell Degrader |
| Protéines cibles | Bromodomain |
| CAS | 1797406-69-9 |
| Formule moléculaire | C<sub>49</sub>H<sub>60</sub>ClN<sub>9</sub>O<sub>8</sub>S<sub>2</sub> |
| Poids de la formule | 1002.64g/mol |
| Contenu et stockage | Store at -20°C |
| À utiliser avec (application) | Bromodomain Inhibitors |
| Quantité | 5 mg |
