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  3. GSK-3β inhibitor 2

GSK-3β inhibitor 2 

Cat. No.: HY-130795
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GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.

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GSK-3β inhibitor 2 Chemical Structure

GSK-3β inhibitor 2 Chemical Structure

CAS No. : 1702428-31-6

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Description

GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

1.1 nM (IC50)

In Vitro

The pyridine carboxamide of GSK-3β inhibitor 2 (Compound 3) makes hydrogen bonds with the hinge V135 backbone amide, and the carbonyl oxygen of the thiazolyl primary amide formed a critical hydrogen bond with K85. The quality of the electron density for the methyl group of the methoxy moiety in GSK-3β inhibitor 2 does not allow its unambiguous placement in the model, but a small molecule crystal structure of GSK-3β inhibitor 2 determined by single crystal X-ray diffraction method confirmed the intramolecular hydrogen bonding between the methoxy -O- and the amide N-H in GSK-3β inhibitor 2[1].

In Vivo

The elevation of hyperphosphorylated Tau (pTau) is mimicked in LaFerla 3xTg-C57BL6 mice, and accordingly, these mice are used as an in vivo model of Alzheimer’s disease. GSK-3β inhibitor 2 (Compound 3) shows a significant reduction in pTau396 when administered orally at 30 mg/kg as a nanosuspension to LaFerla 3xTg-C57BL6 male mice. GSK-3β inhibitor 2 shows only modest brain exposure (B/P = 0.26) as determined as a single time point[1].

Molecular Weight

318.35

Formula

C₁₄H₁₄N₄O₃S

CAS No.

1702428-31-6

SMILES

O=C(C1=C(OC)N=C(C2=CC(NC(C3CC3)=O)=NC=C2)S1)N

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GSK-3β inhibitor 2GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3HyperphosphorylatedTauneurodegenerativeCNSpenetrationBBBAlzheimer'sdiseaseSer396Inhibitorinhibitorinhibit

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GSK-3β inhibitor 2
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HY-130795
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