GSK-3β inhibitor 3

GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β) , with an IC 50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia In Vitro GSK-3β inhibitor 3 (compound 4-3) (100 μM) inhibits GSK-3α activity by 87.3%. GSK-3β inhibitor 3 (6.25-100 μM; 24-48 h) dose-dependently inhibits the growth of NB4 and NB4-R1 cells. GSK-3β inhibitor 3 (12.5-100 μM; 24 h) significantly increases the percentage of apoptosis in a dose-dependent pattern in NB4 and NB4-R1 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: NB4 and NB4-R1 cells Concentration: 6.25, 12.5, 25, 50, 100 μM Incubation Time: 24, 48 hours Result: Inhibited the cell viability, with IC 50 s of 19.56 μM and 26.42 μM in NB4 and NB4-R1 cells at 24 h, respectively. Had little cytotoxicity on human normal liver cells (LO 2 ) and human umbilical vein endothelial cells (HUVECs). Apoptosis AnalysisCell Line: NB4 and NB4-R1 cells Concentration: 12.5, 25, 50, 100 μM Incubation Time: 24 hours Result: Induced cell apoptosis. In Vivo GSK-3β inhibitor 3 (compound 4-3) (15 mg/kg/d; i.p. for 2 weeks) inhibits tumor growth of mice by 75.97% relative to vehicle control . GSK-3β inhibitor 3 (15 mg/kg; a single i.p.) shows long T 1/2 of 14.2 h, high AUC values (AUC last =3503.42 ng/mL•h), and maximum concentration (C max =515 ng/mL) in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c female nude mice were injected leukemia cells Dosage: 15 mg/kg/d Administration: I.p. for 2 weeks Result: Inhibited localized growth in NB4 cells. Had mild weight loss compared with control. Animal Model: Male ICR mice (30 g) Dosage: 15 mg/kg (Pharmacokinetic Analysis) Administration: A single i.p. Result: T 1/2 =14.2 h; AUC last =3503.42 ng/mL•h; C max =515 ng/mL. IC50& Target:GSK-3β 6.6 μM (IC 50 )

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