GSK-3β inhibitor 6

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GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC₅₀ value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.

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

GSK-3β inhibitor 6 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

GSK-3β

24.4 μM (IC₅₀)

In Vitro

GSK-3β inhibitor 6 (Compound B30, 0-30 μΜ, 30 min) shows good GSK-3β kinase inhibitory activity (IC₅₀: 24.4 μM)^[1].
GSK-3β inhibitor 6 (5 μM, 3 h) shows high hepatocyte glucose uptake (38%) with no significant toxicity against HepG2 cells^[1].

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

In Vivo

GSK-3β inhibitor 6 (Compound 5k, oral administration, 20 mg/kg) shows favorable drug-like properties (t_1/2: 1.41 h, C_max: 288 ng/mL)^[2].

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

Animal Model:

Sprague-Dawley rats (pharmacokinetic assay)^[2]

Dosage:

2 mg/kg, 20 mg/kg

Administration:

Intravenous injection (2 mg/kg), oral administration (20 mg/kg)

Result:

Pharmacokinetic profile of GSK-3β inhibitor 6 (Compound 5k).

Compound	Route	Dose (mg/kg)	t_1/2 (h)	Tmax (h)	C_max (ng/mL)	AUC_0-t (hr•ng/mL)	AUC_0-∞ (hr•ng/mL)	CL (mL/hr/kg)	F (%)
GSK-3β inhibitor 6	Oral administration	20	1.41	1.33	288	1030	1073	18719	11.4
GSK-3β inhibitor 6	Intravenous injection	2	2.13	0.08	449	872.89	940.48	2190.83

F: oral bioavailability.

Molecular Weight

393.28

Formula

C₂₀H₁₇BrN₄

SMILES

CC1=CC=CC(C)=C1NC2=NC=CC(C3=CNC4=CC=C(C=C43)Br)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Shuwen Han, et al. Structural-Based Optimizations of the Marine-Originated Meridianin C as Glucose Uptake Agents by Inhibiting GSK-3β. Mar Drugs. 2021 Mar 12;19(3):149. [Content Brief]

[2]. Shuwen Han, et al. Structure-Based design of Marine-derived Meridianin C derivatives as glycogen synthase kinase 3β inhibitors with improved oral bioavailability: From aminopyrimidyl-indoles to the sulfonyl analogues. Bioorg Chem. 2022 Feb;119:105537. [Content Brief]