SGK1-IN-10
SGK1-IN-10 is an ATP-competitive SGK1 inhibitor with an IC50 of 2.53 μM against human SGK1, and it exhibits blood-brain barrier permeability. SGK1-IN-10 downregulates the phosphorylation levels of MDM2 and GSK-3β, induces apoptosis and inhibits cell migration. SGK1-IN-10 can be used in the research of prostate cancer.
For research use only. We do not sell to patients.
- Formula: C24H27F3N4O
- Molecular Weight:444.49
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
SGK1 2.53 μM (IC50) |
SGK1-IN-10 (compound 7h) inhibits proliferation of PC3 prostate cancer cells with an IC50 of 1.08 μM and LNCaP prostate cancer cells with an IC50 of 1.24 μM[1].
SGK1-IN-10 inhibits proliferation of HepG2 liver cancer cells with an IC50 of 1.21 μM and shows low cytotoxicity to LX2 normal liver cells with an IC50 of 10.07 μM, yielding a selectivity index of 9.15[1].
SGK1-IN-10 (0.5-2.0 μM; 48 h) induces concentration-dependent apoptosis in PC3 prostate cancer cells, with a total apoptotic rate of 74.70% at 2.0 μM[1].
SGK1-IN-10 (0.5-2.0 μM; 48 h) induces concentration-dependent S-phase cell cycle arrest in PC3 prostate cancer cells, with 61.48% of cells in S-phase at 2.0 μM[1].
SGK1-IN-10 (0.5-2.0 μM; 24-48 h) inhibits migration of PC3 prostate cancer cells in a dose- and time-dependent manner[1].
SGK1-IN-10 (0.01-10 μM; 2 h) directly binds to and stabilizes SGK1 protein in PC3 prostate cancer cells in a temperature- and concentration-dependent manner[1].
SGK1-IN-10 (0.5-2.0 μM) dose-dependently inhibits phosphorylation of SGK1 substrates MDM2 and GSK-3β in PC3 prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PC3 prostate cancer cells
-
Concentration:0.5 μM, 1.0 μM, 2.0 μM
-
Incubation Time:48 h
-
Result:Increased total apoptotic rate to 19.64% at 0.5 μM compared to 5.97% in DMSO control.
Increased total apoptotic rate to 28.19% at 1.0 μM compared to 5.97% in DMSO control.
Increased total apoptotic rate to 74.70% at 2.0 μM compared to 5.97% in DMSO control.
-
Cell Line:PC3 prostate cancer cells
-
Concentration:0.5 μM, 1.0 μM, 2.0 μM
-
Incubation Time:48 h
-
Result:Increased S-phase population to 49.59% at 0.5 μM compared to 22.60% in DMSO control.
Increased S-phase population to 59.40% at 1.0 μM compared to 22.60% in DMSO control.
Increased S-phase population to 61.48% at 2.0 μM compared to 22.60% in DMSO control.
-
Cell Line:PC3 prostate cancer cells
-
Concentration:0.5 μM, 1.0 μM, 2.0 μM
-
Incubation Time:24 h, 48 h
-
Result:Inhibited wound closure in a dose- and time-dependent manner.
Showed significant inhibition at all concentrations at 24 h compared to DMSO control.
Showed significant inhibition at all concentrations at 48 h compared to DMSO control.
Chemical Information
-
Molecular Weight 444.49
-
Formula C24H27F3N4O
-
SMILES
FC(C1=CC(NC2=CC=C(CN3C[C@H](C)N[C@H](C)C3)C=C2)=NC4=CC=C(OC)C=C14)(F)F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
Powered by Bioz