2. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage Neuronal Signaling
  3. GSK-3 CDK Tau Protein
  4. GSK-3 inhibitor 3

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.

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GSK-3 inhibitor 3 Chemical Structure

GSK-3 inhibitor 3 Chemical Structure

CAS No. : 2227279-84-5

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Based on 1 publication(s) in Google Scholar

GSK-3 inhibitor 3 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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  • Purity & Documentation

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Description

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].

IC50 & Target[1]

GSK-3α

0.35 nM (IC50)

GSK-3β

0.25 nM (IC50)

CDK2

0.22 μM (IC50)

CDK5

1.3 μM (IC50)

In Vitro

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].

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

GSK-3 inhibitor 3 Related Antibodies
In Vivo

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]

>Tmax (h)

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

Route Dose (mg/kg) CL (mL•min-1/kg-1) Vss (L/kg) MRT (h) T1/2 (h) AUCtot (μM/h) Cmax (μM) F (%)
i.v. 2 23.3 5.4 3.9 2.5 / / /
p.o. 10 / / / / 24.3 3.5 ~100
Animal Model: Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.)
Result: Produced a 37% reduction in pTau396.
Molecular Weight

410.40

Formula

C23H15FN6O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CC=C(C2=C(C=NC=C2)NC(C3=CC=NC(NC4=CC=C(C#N)C=C4)=N3)=O)C=C1
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 : 50 mg/mL (121.83 mM; Need ultrasonic; 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 2.4366 mL 12.1832 mL 24.3665 mL
5 mM 0.4873 mL 2.4366 mL 4.8733 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  15% Cremophor EL    85% Saline

    Solubility: 1.5 mg/mL (3.65 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  17% Solutol HS-15 in Saline

    Solubility: 0.83 mg/mL (2.02 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
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 2.4366 mL 12.1832 mL 24.3665 mL 60.9162 mL
5 mM 0.4873 mL 2.4366 mL 4.8733 mL 12.1832 mL
10 mM 0.2437 mL 1.2183 mL 2.4366 mL 6.0916 mL
15 mM 0.1624 mL 0.8122 mL 1.6244 mL 4.0611 mL
20 mM 0.1218 mL 0.6092 mL 1.2183 mL 3.0458 mL
25 mM 0.0975 mL 0.4873 mL 0.9747 mL 2.4366 mL
30 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0305 mL
40 mM 0.0609 mL 0.3046 mL 0.6092 mL 1.5229 mL
50 mM 0.0487 mL 0.2437 mL 0.4873 mL 1.2183 mL
60 mM 0.0406 mL 0.2031 mL 0.4061 mL 1.0153 mL
80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7615 mL
100 mM 0.0244 mL 0.1218 mL 0.2437 mL 0.6092 mL
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GSK-3 inhibitor 3 Related Classifications

Help & FAQs
  • 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-3 inhibitor 32227279-84-5GSK-3CDKTau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseGSK-3 inhibitorCDK inhibitorADAlzheimer’s disease modelInhibitorinhibitorinhibit

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