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Cat. No.: HY-154851

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GSK-3 inhibitor 3

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Based on 1 Customer Validation

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.

For research use only. We do not sell to patients.

Purity: 99.10%
CAS No.: 2227279-84-5
Formula: C₂₃H₁₅FN₆O
Molecular Weight:410.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK-3 inhibitor 3 Chemical Structure

CAS No.: 2227279-84-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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)

All GSK-3 Isoforms :

All CDK Isoforms :

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.

In Vivo

GSK-3 inhibitor 3 (2 mg.kg for i.v., 10 mg/kg for p.o.) shows a T_1/2 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]
>T_max (h)

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

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.

Chemical Information

CAS No. 2227279-84-5
Appearance Solid
Molecular Weight 410.40
Formula C₂₃H₁₅FN₆O
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

Route	Dose (mg/kg)	CL (mL•min^-1/kg^-1)	V_ss (L/kg)	MRT (h)	T_1/2 (h)	AUC_tot (μM/h)	C_max (μM)	F (%)
i.v.	2	23.3	5.4	3.9	2.5	/	/	/
p.o.	10	/	/	/	/	24.3	3.5	~100

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4366 mL

12.1832 mL

24.3665 mL

5 mM

0.4873 mL

2.4366 mL

4.8733 mL

10 mM

0.2437 mL

1.2183 mL

2.4366 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hartz RA, et.al. Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors. J Med Chem. 2023 Jun 8;66(11):7534-7552. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References

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GSK-3 inhibitor 3

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

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Antidepressant Compound Library

Anti-Pulmonary Fibrosis Compound Library

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Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

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Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

All GSK-3 Isoforms

All CDK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK-3 inhibitor 3 Related Classifications

HY-154851 Related Classifications