GSK-3β inhibitor 3 是一种有效，选择性，不可逆和共价的糖原合酶激酶 3β (GSK-3β) 抑制剂，IC50 值为 6.6 μM。GSK-3β inhibitor 3 可用于急性早幼粒细胞白血病的研究。
货号:ajcx33524
CAS:1448990-73-5
分子式:C18H14FNO2S
分子量：327.37
溶解度:DMSO : 250 mg/mL (763.66 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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/mL?h), and maximum concentration (Cmax=515 ng/mL) in mice[1].

[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.