1. PI3K/Akt/mTOR Stem Cell/Wnt Neuronal Signaling JAK/STAT Signaling TGF-beta/Smad Epigenetics
  2. GSK-3 Tau Protein AAK1 Pim PKC
  3. GSK-3β inhibitor 13

GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease.

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GSK-3β inhibitor 13 Chemical Structure

GSK-3β inhibitor 13 Chemical Structure

CAS No. : 2227316-74-5

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Description

GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

0.73 nM (IC50)

GSK-3α

0.35 nM (IC50)

PKCθ

0.36 μM (IC50)

PIM1

0.38 μM (IC50)

AAK1

0.20 μM (IC50)

In Vivo

GSK-3β inhibitor 13 has an exposure of 3.8 μM in plasma and 1.3 μM in brain, resulting in a brain-to-plasma (B/P) ratio of 0.34[1].
GSK-3β inhibitor 13 (30 mg/kg; p.o.; single dose) results in a 52% reduction in pTau396 in in LaFerla 3xTg-C57BL6 mice[1].

Pharmacokinetic Analysis in Mice[1]

Route Dose (mg/kg) CL (mL/mL/kg) Vss (L/kg) MRT (h) t1/2 (h)
i.v. 2 3.8 1.1 4.8 5.2
Route Dose (mg/kg) AUCtot (μM·h) Cmax (μM) F (%)
p.o. 10 68.3 7.8 64

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

414.46

Formula

C23H22N6O2

CAS No.
SMILES

O=C(C1=CC=NN2C1=NC(C3=CC=CC=C3)=C2)NC4=C(C=CN=C4)N5CCOC(C5)C

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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GSK-3β inhibitor 13
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HY-149054
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