MZ1 是由 von Hippel-Lindau 和 BRD4 的配体连接的 PROTAC。 MZ1 比 BRD2 和 BRD3 有效且快速地诱导 BRD4 的可逆、持久和选择性去除。 BRD4 BD1/2、BRD3 BD1/2 和 BRD2 BD1/2 的 Kd 分别为 382/120、119/115 和 307/228 nM。
| Cas No. | 1797406-69-9 |
| 化学名 | (4R)-N-[14-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-1,13-dioxo-3,6,9-trioxa-12-azatetradec-1-yl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide |
| Canonical SMILES | CC1=NN=C2[C@H](CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N3[C@H](C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)C[C@@H](O)C3)=O)=O)=O)N=C(C6=CC=C(Cl)C=C6)C7=C(SC(C)=C7C)N21 |
| 分子式 | C49H60ClN9O8S2 |
| 分子量 | 1002.6 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH7.2) (1:7): 0.12 mg/mL |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4). It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ-1, which binds bromo- and extra-terminal (BET) proteins, linked to a ligand for the E3 ubiquitin ligase VHL. MZ1 induces the selective degradation of BRD4 in HeLa cells when used at 0.1-0.5 uM. At concentrations of 2-10 uM, MZ1 causes the removal of BRD2, BRD3, and BRD4. BRD protein removal is evident within four hours of adding MZ1 and persists for at least 48 hours, unless MZ1 is removed. |
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