PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 是一种基于 von Hippel-Lindau 配体的 SKG3 降解剂。 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
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PROTAC SGK3 degrader-1
CAS number：2381320-35-8 molecular formula：C57H73FN10O11S2
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| Chinese alias | - | ||
| English alias | SGK3-PROTAC1 | ||
| CAS number | 2381320-35-8 | molecular formula | C57H73FN10O11S2 |
| molecular weight | 1157.38 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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