Cat. No.: HY-149054

GSK-3β inhibitor 13

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Based on 1 Customer Validation

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.

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

Purity: 99.74%
CAS No.: 2227316-74-5
Formula: C₂₃H₂₂N₆O₂
Molecular Weight:414.46

Storage:

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

GSK-3β inhibitor 13 Chemical Structure

CAS No.: 2227316-74-5

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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 Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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)

All GSK-3 Isoforms :

All Pim Isoforms :

All PKC Isoforms :

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)	V_ss (L/kg)	MRT (h)	t_1/2 (h)
i.v.	2	3.8	1.1	4.8	5.2
Route	Dose (mg/kg)	AUC_tot (μM·h)	C_max (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.

Chemical Information

CAS No. 2227316-74-5
Appearance Solid
Molecular Weight 414.46
Formula C₂₃H₂₂N₆O₂
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)

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

2.4128 mL

12.0639 mL

24.1278 mL

5 mM

0.4826 mL

2.4128 mL

4.8256 mL

10 mM

0.2413 mL

1.2064 mL

2.4128 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)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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. Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-b]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors. J Med Chem. 2023 Mar 23;66(6):4231-4252. [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	2.4128 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

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All GSK-3 Isoforms

All Pim Isoforms

All PKC Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK-3β inhibitor 13 Related Classifications

HY-149054 Related Classifications