PROTAC SGK3 degrader-2
PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878). PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1 and S6K1, with IC50 values of 0.6 μM, 1.4 μM and 1.7 μM, respectively, but fails to degrade SGK3. PROTAC SGK3 degrader-2 can serve as a control compound to investigate the specific effects of SGK3 degradation mediated by SGK3-PROTAC1.
(Pink: SGK3 ligand (HY-151009); Blue: VHL ligand (HY-120217A); Black: linker (HY-130618)).
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- CAS. Nr.: 2381196-78-5
- Formel: C57H73FN10O11S2
- Molecular Weight:1157.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
SGK1 1.4 μM (IC50) |
SGK3 0.6 μM (IC50) |
In Vitro
PROTAC SGK3 degrader-2 (cisSGK3-PROTAC1) inhibits purified SGK3, SGK1 and S6K1 kinases in cell-free assays, with IC50 values of 0.6 μM, 1.4 μM and 1.7 μM, respectively[1].
PROTAC SGK3 degrader‑2 (0.03‑3 μM; 8 h) co‑treated with either AZD5363 (HY‑15431) does not reduce the phosphorylation level of NDRG1‑Thr346 in HEK293 cells[1].
PROTAC SGK3 degrader-2 (0.03-3 μM; 14 h) fails to induce SGK3 degradation in CAMA‑1, ZR‑75‑1 and JIMT‑1 breast cancer cell lines[1].
PROTAC SGK3 degrader‑2 (0.3 μM; 5 days) combined with either GDC0941 (HY‑50094) or AZD5363 exerts no significant effect on SGK3 protein levels and its downstream mTORC1 signaling pathway in CAMA‑1 and ZR‑75‑1 cells[1].
PROTAC SGK3 degrader-2 (0.3 μM; up to 4 weeks) barely enhances the growth inhibitory effect of PI3K/Akt inhibitors on CAMA-1 and ZR-75-1 breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:8 h
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Result:Did not reduce NDRG1‑Thr346 phosphorylation in HEK293 cells under the condition of AZD5363 co‑treatment.
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Cell Line:CAMA-1, ZR-75-1, and JIMT-1 breast cancer cells
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Concentration:0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:14 h
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Result:Failed to induce SGK3 degradation in CAMA‑1, ZR‑75‑1 and JIMT‑1 breast cancer cell lines.
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Cell Line:CAMA-1 and ZR-75-1 breast cancer cells
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Concentration:0.3 μM (combined with 1 μM GDC0941 or 1 μM AZD5363)
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Incubation Time:8 h or 5 days
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Result:Exerted no obvious influence on SGK3 protein level and downstream mTORC1 signalling when combined with GDC0941 or AZD5363 in CAMA‑1 and ZR‑75‑1 cells.
Chemical Information
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CAS. Nr. 2381196-78-5
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Molecular Weight 1157.38
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Formel C57H73FN10O11S2
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SMILES
O=C(N1[C@@H](C[C@@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOCCOCCCCCCN(CCO4)C[C@@H]4COC5=C(C=NN6)C6=NC(C7=CC=C(C=C7)NS(=O)(C8=C(C=CC(C)=C8)F)=O)=N5)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PROTAC SGK3 degrader-2 Related Classifications
HY-176823 Related Classifications
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