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^[1].

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.

SGK1-IN-8 (compound 55) (5-10 mg/kg; i.p., p.o.; single dose) shows rapid absorption after single i.p. or p.o. administration in male BALB/c mice, with low brain penetration resulting in a brain-Kp (AUC_last) of 0.04 for both routes^[1].

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

336.78

C₁₈H₁₃ClN₄O

3109982-48-8

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Madruga E, et al. Brain Permeable SGK1 Inhibitors: A Promising Therapeutic Strategy for Neurodegenerative Diseases. J Med Chem. 2026;69(6):6790-6815.  [Content Brief]