GSK-3β inhibitor 3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.Cell Viability Assay Cell 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 IC50s 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 (LO2) and human umbilical vein endothelial cells (HUVECs).Apoptosis Analysis Cell Line:NB4 and NB4-R1 cells Concentration:12.5, 25, 50, 100 μM Incubation Time:24 hours Result:Induced cell apoptosis.

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 T1/2 of 14.2 h, high AUC values (AUClast=3503.42 ng/mL?h), and maximum concentration (Cmax=515 ng/mL) in mice.Animal Model:Balb/c female nude mice were injected leukemia cellsDosage: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:T1/2=14.2 h; AUClast=3503.42 ng/mL?h; Cmax=515 ng/mL.

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Apoptosis

Apoptosis

Apoptosis | GSK-3

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1448990-73-5

327.37

C18H14FNO2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (763.66 mM; 超声助溶 )

Fc1ccc(cc1)C1CC(=O)N(C(=O)C=C)c2ccccc2S1

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(-20℃)

With Ice Pack

≥ 2 years