GSK-3 inhibitor 3

• CAT Number: I041059
• CAS Number: 2227279-84-5
• Purity: ≥95%
• Synonyms: 2-(4-cyanoanilino)-N-[4-(4-fluorophenyl)pyridin-3-yl]pyrimidine-4-carboxamide
• InChI: InChI=1S/C23H15FN6O/c24-17-5-3-16(4-6-17)19-9-11-26-14-21(19)29-22(31)20-10-12-27-23(30-20)28-18-7-1-15(13-25)2-8-18/h1-12,14H,(H,29,31)(H,27,28,30)
• InChIKey: QLWFPXXGZGCHFQ-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1C#N)NC2=NC=CC(=N2)C(=O)NC3=C(C=CN=C3)C4=CC=C(C=C4)F

GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research[1].
GSK-3 inhibitor 3 (Compound 34) (1 μM) is a highly selective inhibitor of CDK2 and CDK5, with IC50s of 0.22 μM and 1.3 μM for CDK2 and CDK5, respectively[1].
GSK-3 inhibitor 3 (2 mg.kg for i.v., 10 mg/kg for p.o.) shows a T1/2 of 2.5 h (i.v.), and oral bioavailability (F%) of ~100% in male C57BL6 mice [1].
GSK-3 inhibitor 3 (10 mg/kg for p.o.; only once) produces a 33% reduction in pTau396 in Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice [1].
Pharmacokinetic parameters for GSK-3 inhibitor 3(Compound 34) in Mice[1]

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