SGK1-IN-8
SGK1-IN-8 (compound 55) is a SGK1 and GSK3β inhibitor, with an IC50 of 0.11 μM against human SGK1 and an IC50 of 3.39 μM against human GSK3β. SGK1-IN-8 inhibits the catalytic activities of SGK1 and GSK3β, and reduces the phosphorylation level of TAU protein at the Ser214 site. SGK1-IN-8 is available for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 3109982-48-8
- Formula: C18H13ClN4O
- Molecular Weight:336.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
SGK1-IN-8 (variable concentrations; 1 h) potently inhibits human recombinant SGK1 with an IC50 of 0.11 μM[1].
SGK1-IN-8 (1 μM; 1 h pre-incubation, 24 h total with OA) is non-toxic to SH-SY5Y cells and provides statistically significant neuroprotection against okadaic acid-induced toxicity[1].
SGK1-IN-8 (1 μM) does not change total TAU levels but significantly reduces TAU phosphorylation at Ser396 and Ser214 in SH-SY5Y cells[1].
SGK1-IN-8 (10 μM; 120 min) is a P-glycoprotein substrate, as demonstrated by an efflux ratio of 2.90 in MDR1-transfected MDCKII cells that is reversed by the P-gp inhibitor Zosuquidar (HY-15255)[1].
SGK1-IN-8 (variable concentrations; 30 min) weakly inhibits human recombinant GSK3β with an IC50 of 3.39 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y human neuroblastoma cells (okadaic acid-induced AD model)
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Concentration:1 μM (compound 55)
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Incubation Time:1 h pre-incubation; 24 h total incubation with OA
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Result:Showed no significant reduction in cell viability at 1 μM, and statistically significantly restored cell viability in OA-treated SH-SY5Y cells, indicating neuroprotective activity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3109982-48-8
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Molecular Weight 336.78
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Formula C18H13ClN4O
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SMILES
O=C(C1=CNC=C1C2=CC=C(Cl)C=C2)NC3=CC4=C(NN=C4)C=C3
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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)