PROTAC Mcl1 degrader-1 (compound C3) 是一种靶向嵌合体的蛋白水解 (PROTAC)，是有效，选择性的 Mcl-1 抑制剂，IC50 为 0.7 μM。PROTAC Mcl1 degrader-1 通过将具有微摩尔范围亲和力的 E3 连接酶脑 (CRBN) 结合配体 pomalidomide 引入 Mcl-1 抑制剂 S1-6 来诱导 Mcl-1 的泛素化和蛋白酶体降解。
| Cas No. | 2163793-38-0 |
| Canonical SMILES | O=C(C1=CC=CC(NCCCCCCNC(CCCCC(NCCN2C(C3=C4C(C2=O)=CC=C(C4=CC=C3)SC5=CC=C(C=C5)Br)=O)=O)=O)=C1C6=O)N6C7CCC(NC7=O)=O |
| 分子式 | C45H45BrN6O8S |
| 分子量 | 909.84 |
| 溶解度 | DMSO: 50 mg/mL (54.95 mM) |
| 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 | PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity[1]. [1]. Wang Z, et al. Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands. J Med Chem. 2019 Aug 21. |
