GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia[1].
GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia[1].
GSK-3β inhibitor 3 (compound 4-3) (100 μM) inhibits GSK-3α activity by 87.3%[1].GSK-3β inhibitor 3 (6.25-100 μM; 24-48 h) dose-dependently inhibits the growth of NB4 and NB4-R1 cells[1].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[1].
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[1].GSK-3β inhibitor 3 (15 mg/kg; a single i.p.) shows long T1/2 of 14.2 h, high AUC values (AUClast=3503.42 ng/mLh), and maximum concentration (Cmax=515 ng/mL) in mice[1].
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[1].
GSK-3β inhibitor 3 (15 mg/kg; a single i.p.) shows long T1/2 of 14.2 h, high AUC values (AUClast=3503.42 ng/mLh), and maximum concentration (Cmax=515 ng/mL) in mice[1].
| Animal Model: | Balb/c female nude mice were injected leukemia cells[1] |
| 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)[1] |
| Dosage: | 15 mg/kg (Pharmacokinetic Analysis) |
| Administration: | A single i.p. |
| Result: | T1/2=14.2 h; AUClast=3503.42 ng/mLh; Cmax=515 ng/mL. |
[1]. Zhang P, et, al. Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. J Med Chem. 2021 May 24.
