PROTAC SGK3降解剂-1
规格
| Cas Number | 2381320-35-8 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 10mg 或 1mg 或 5mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (86.4 mM); Ethanol: 100 mg/mL (86.4 mM); Water: Insoluble; |
| 简短描述 | SGK抑制剂 |
| 英文简短描述 | SGK Inhibitors |
| 过滤标签 | 羟基聚乙二醇,PROTACs,SGK,Metabolic Enzyme/Protease,PROTAC,PROTAC linker,SGK inhibitor,DBCO PEG,Aliphatic Linkers |
| 储存温度 | -20°C储存,充氩 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是 308-R SGK 抑制剂与 VH032 VHL 结合配体的 PROTAC 共轭物，可靶向降解 SGK3（血清/糖皮质激素调节激酶家族成员 3）。 |
| 描述 |
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是一种基于 von Hippel-Lindau 配体的 SKG3 降解剂。 |
| 英文描述 |
Information PROTAC SGK3 degrader-1 PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family Member 3) for degradation. Targets SGK3 In vitro SGK3-PROTAC1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 h, with maximal 80% degradation observed within 8 h, accompanied by a loss of phosphorylation of NDRG1, an SGK3 substrate. Low doses of SGK3-PROTAC1 (0.1−0.3 μM) restores sensitivity of SGK3 dependent ZR-75-1 and CAMA-1 breast cancer cells to Akt and PI3K inhibitors, whereas the cis epimer analogue incapable of binding to the VHL E3 ligase has no impact. SGK3-PROTAC1 suppresses proliferation of ZR-75-1 and CAMA-1 cancer cell lines treated with a PI3K inhibitor more effectively than could be achieved by a conventional SGK isoform inhibitor. Cell Research(from reference) Cell lines：CAMA-1, HEK293 cells Concentrations：0.3 μM Incubation Time：8 h |