1. Metabolic Enzyme/Protease Neuronal Signaling
  2. SGK Tau Protein
  3. SGK1-IN-7

SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid (HY-N6785). SGK1-IN-7 can be used in the research of Alzheimer's disease.

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SGK1-IN-7

SGK1-IN-7 Chemical Structure

CAS No. : 3109982-58-0

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Description

SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid (HY-N6785). SGK1-IN-7 can be used in the research of Alzheimer's disease[1].

In Vitro

SGK1-IN-7 (Compound 102) (6.25-50 μM; 30 min) is non-mutagenic and has a low cardiac safety risk, with no significant inhibition of hERG or Nav1.5 channels and moderate Cav1.2 inhibition (IC50 = 12.1 μM)[1].
SGK1-IN-7 (5 μM; 24 h) exerts significant neuroprotective effects in Okadaic acid-treated SH-SY5Y human neuroblastoma cells at 5 μM[1].
SGK1-IN-7 (5 μM; 24 h) significantly reduces phosphorylation of tau at Ser396 and Ser214 sites in SH-SY5Y human neuroblastoma cells at 5 μM without altering total tau levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SH-SY5Y human neuroblastoma cells
Concentration: 5 μM
Incubation Time: 24 h (OA pre-treatment)
Result: Significantly restored cell viability in OA-treated SH-SY5Y cells, showing a statistically significant neuroprotective effect compared to OA-only treatment.
Parmacokinetics
Species Dose Route Tmax (Plasma) AUClast T1/2 Bioavailability
Mice[1] 2.5 mg/kg i.v. / 954.87 ng·h/mL 0.93 h /
Mice[1] 5 mg/kg i.p. 0.25 h 793.15 1.24 h /
Mice[1] 10 mg/kg p.o. 0.50 h 806.97 ng·h/mL 1.83 h 21 %
In Vivo

SGK1-IN-7 (Compound 102) (2.5-10 mg/kg; i.v., i.p., p.o.; single dose) exhibits dose-dependent plasma and brain exposure in male BALB/c mice, with brain-plasma ratios (brain-Kp) of 0.49, 0.18, and 0.25 following i.v., i.p., and p.o. single-dose administration, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

385.25

Formula

C19H14Cl2N4O

CAS No.
SMILES

O=C(C1=CN(C)C=C1C2=CC=C(Cl)C(Cl)=C2)NC3=CC4=C(NN=C4)C=C3

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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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SGK1-IN-7
Cat. No.:
HY-182323
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