2. PI3K/Akt/mTOR Stem Cell/Wnt Neuronal Signaling JAK/STAT Signaling TGF-beta/Smad Epigenetics
  3. GSK-3 Tau Protein AAK1 Pim PKC
  4. 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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Based on 1 publication(s) in Google Scholar

GSK-3β inhibitor 13 Related Antibodies

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PIM1 PIM2 PIM3

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (60.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4128 mL 12.0639 mL 24.1278 mL
5 mM 0.4826 mL 2.4128 mL 4.8256 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4128 mL 12.0639 mL 24.1278 mL 60.3195 mL
5 mM 0.4826 mL 2.4128 mL 4.8256 mL 12.0639 mL
10 mM 0.2413 mL 1.2064 mL 2.4128 mL 6.0319 mL
15 mM 0.1609 mL 0.8043 mL 1.6085 mL 4.0213 mL
20 mM 0.1206 mL 0.6032 mL 1.2064 mL 3.0160 mL
25 mM 0.0965 mL 0.4826 mL 0.9651 mL 2.4128 mL
30 mM 0.0804 mL 0.4021 mL 0.8043 mL 2.0106 mL
40 mM 0.0603 mL 0.3016 mL 0.6032 mL 1.5080 mL
50 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2064 mL
60 mM 0.0402 mL 0.2011 mL 0.4021 mL 1.0053 mL
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GSK-3β inhibitor 13 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK-3β inhibitor 132227316-74-5GSK-3Tau ProteinAAK1PimPKCGlycogen synthase kinase-3Glycogen synthase kinase 3Adaptor-associated Kinase 1AP2-associated kinase 1Pim kinasesProtein kinase CInhibitorinhibitorinhibit

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