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.
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- CAS No.: 3046378-98-4
- 화학식: C30H30F3N5O4
- 분자량:581.59
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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SGK1 0.39 μM (IC50) |
SGK2 1.76 μM (IC50) |
SGK3 1.95 μM (IC50) |
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.
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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분자량 581.59
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)