GSK-3 inhibitor 4

Research use only, not for human use.

GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5).

GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies.

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Animal Model:3xTg mice were bred onto the C57BL6 background and bred as homozygotes. Male animals between the ages of five to seven months were used for the study.Dosage:10 mg/kgAdministration:Oral gavage (p.o.) Result:Produced a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg.Animal Model:male C57BL6 mice (Pharmacokinetic assay)Dosage:2 mg/kg, 10 mg/kg. Administration: Kept for 8 h fasting prior to formulation administration. intravenous and oral routes of administration to mice at a dose of 2 and 10 mg/kg, respectively.Result:Exhibited clearance ranging from 15.8 to 23.3 mL /min/kg , halflives ranging from 2.5 to 2.9 h and were readily orally bioavailable (F% = 53).

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PI3K/Akt/mTOR signaling

GSK-3

GSK-3 | CDK

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2227279-83-4

403.38

C22H15F2N5O

>98% (HPLC)

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N(C(=O)C1=NC(NC2=CC=C(F)C=C2)=NC=C1)C=3C(=CC=NC3)C4=CC=C(F)C=C4

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(-20℃)

With Ice Pack

≥ 2 years