SGK1-IN-6
SGK1-IN-6 is a selective SGK1 inhibitor with an IC50 of 0.39 μM, showing selectivity over SGK2/3. SGK1-IN-6 inhibits cancer cell migration and invasion, improves SGK1 protein thermal stability. SGK1-IN-6 decreases SGK1 protein levels in tumor tissues, suppresses tumor growth in mouse xenograft models. SGK1-IN-6 can be used for the research of prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 3046378-98-4
- Formula: C30H30F3N5O4
- Molecular Weight:581.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
SGK1 0.39 μM (IC50) |
SGK2 1.76 μM (IC50) |
SGK3 1.95 μM (IC50) |
In Vitro
SGK1-IN-6 (compound 12f) (0.1-1 μM; 24-48 h) inhibits cell migration in PC3 cells in a dose dependent manner[1].
SGK1-IN-6 (0.1-1 μM; 24-48 h) inhibits cell invasion in PC3 cells in a dose dependent manner[1].
SGK1-IN-6 (0.01-10 μM; 2 h) can target SGK1 protein enrichment in living cells by
enhancing the thermal stability of the target protein SGK1[1].
SGK1-IN-6 (0.05-2 μM; 0-48 h) inhibits SGK1 and its substrate phosphorylation in time- and concentration-dependent manner in PC3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:0.1; 0.5; 1 μM
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Incubation Time:24; 48 h
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Result:Showed varying degrees of reduction compared to the DMSO group at 0.5 μM and 1 μM, by 24 h.
Significantly decreasedcell migration rates in all groups, by 48 h.
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Cell Line:PC3 cells
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Concentration:0.1; 0.5; 1 μM
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Incubation Time:24 h
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Result:Demonstrate significant concentration-dependent inhibition of PC3 cell invasion.
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Cell Line:PC3 cells
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Concentration:0.05; 0.1; 0.5; 1; 2 μM
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Incubation Time:0; 6; 12; 24; 32; 48 h
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Result:Revealed a time-dependent inhibition of NEDD4-2, MDM2, GSK3β, NDRG1, and
SGK1 phosphorylation in PC3 cells.
Showed a time-dependent inhibition of NEDD4-2, MDM2, GSK3β, NDRG1, and
SGK1 phosphorylation in PC3 cells.
Suppressed SGK1 protein and phosphorylation in PC3 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude
mice (4-6 weeks) subcutaneously inoculated PC3 cells[1] -
Dosage:0.5; 2 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Inhibited tumor grwoth at 0.5 and 2 mg/kg doses.
Exerted minimal in vivo toxicity and did not affect organ morphology in mice.
Showed no body weight changes in each experimental group of mice.
Chemical Information
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CAS No. 3046378-98-4
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Molecular Weight 581.59
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Formula C30H30F3N5O4
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SMILES
O=C(C1=CC2=C(C(F)(F)F)C=C(NC3=CC=C(N4CCNCC4)C=C3OC)N=C2C=C1OC)NC5=CC=C(C=C5)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)