GSK-3β inhibitor 6 is a highly potent inhibitor of GSK-3β with an IC50 value of 24.4 μM, significantly enhancing hepatocyte glucose uptake (38%). This compound holds great potential for studying diseases such as diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder [1].

GSK-3β:24.4 μM

GSK-3β inhibitor 6 (Compound B30, 0-30 μM, 30 min) effectively inhibits GSK-3β kinase (IC50: 24.4 μM) and significantly enhances hepatocyte glucose uptake by 38% (5 μM, 3 h) without notable toxicity to HepG2 cells [1].

GSK-3β inhibitor 6 (Compound 5k), administered orally at 20 mg/kg, exhibits favorable pharmacokinetics with a half-life (t1/2) of 1.41 hours and a peak concentration (Cmax) of 288 ng/mL in Sprague-Dawley rats. Pharmacokinetic assessment comparing intravenous injection at 2 mg/kg and oral delivery at 20 mg/kg shows that oral administration results in a t1/2 of 1.41 hours, time to peak concentration (Tmax) of 1.33 hours, and oral bioavailability (F) of 11.4%. In contrast, intravenous injection demonstrates a longer t1/2 of 2.13 hours and a quicker Tmax of 0.08 hours, highlighting the effect of administration routes on the pharmacokinetic profile.