GSK-3β inhibitor 1

Name: GSK-3β inhibitor 1
Brand: MedChemExpress
SKU: HY-126144
Rating: 5.0 (4 reviews)

Cat. No.: HY-126144 Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

GSK-3β inhibitor 1 (compound 3a) inhibits GSK-3β with an IC₅₀ of 4.19 nM. GSK-3β inhibitor 1 demonstrates high antidiabetic efficacy in obese Streptozotocin (HY-13753)-treated rats.

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

GSK-3β inhibitor 1 Chemical Structure

CAS No. : 187325-53-7

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of GSK-3β inhibitor 1:

(E/Z)-GSK-3β inhibitor 1 Get quote

3 Publications Citing Use of MCE GSK-3β inhibitor 1

: GSK-3β inhibitor 1 purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2019 Jun 24;13:2057-2066. [Abstract]; MLTC-1 cells are treated with Rg3 (0, 10, 20 μM) or Rg3 (20 μM) plus GSK3β inhibitor 1 (20 nM) for 24 hrs. Expression level of GSK3β in MLTC-1 cells is detected with Western blotting. The relative expression of GSK3β is quantified via normalization to β-actin.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

GSK-3β inhibitor 1 (compound 3a) inhibits GSK-3β with an IC₅₀ of 4.19 nM. GSK-3β inhibitor 1 demonstrates high antidiabetic efficacy in obese Streptozotocin (HY-13753)-treated rats^[1].

IC₅₀ & Target^[1]

GSK-3β

4.9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	47.97 μM Compound: 3a	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 30902399]

In Vitro

GSK-3β inhibitor 1 is found to effectively occupy hydrophobic cleft of the allosteric binding site. ^[1].
GSK-3β inhibitor 1 (0.1,1,10 μM, 24 h) is nontoxic against PBMCs^[1].
GSK-3β inhibitor 1 (1.56-100 μM, 72 h) inhibits proliferation of A549 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	human PBMCs
Concentration:	0.1,1,10 μM
Incubation Time:	24 h
Result:	Was nontoxic against PBMCs even at concentrations that are much higher than respective IC₅₀ value in functional GSK-3β assay.

Cell Cytotoxicity Assay^[1]

Cell Line:	A549 cells
Concentration:	1.56 -100 μM
Incubation Time:	72 h
Result:	Inhibited proliferation of A549 cells with IC₅₀ of 47.97 μM.

In Vivo

GSK-3β inhibitor 1 (50 mg/kg, i.p., 30 min prior to glucose challenge) effectively prevents increase in blood glucose levels in HFD+STZ diabetic rats^[1].

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

Animal Model:	HFD+STZ diabetic rats ^[1].
Dosage:	50 mg/kg
Administration:	i.p., 30 min prior to glucose challenge
Result:	Vehicle-treated diabetic rats developed persistent hyperglycemic response. Administration of GSK-3β inhibitor 1 30 min prior to glucose challenge effectively prevented increase in blood glucose levels.

Molecular Weight

222.25

Formula

C₁₄H₁₀N₂O

CAS No.

187325-53-7

Appearance

Solid

Color

Yellow to orange

SMILES

O=C1NC2=CC=CC=C2/C1=C/C3=NC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (149.97 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	4.4994 mL	22.4972 mL	44.9944 mL
5 mM	0.8999 mL	4.4994 mL	8.9989 mL
10 mM	0.4499 mL	2.2497 mL	4.4994 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.04%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (256 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Lozinskaya NA, et al. Synthesis and biological evaluation of 3-substituted 2-oxindole derivatives as new glycogen synthase kinase 3β inhibitors. Bioorg Med Chem. 2019 May 1;27(9):1804-1817. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.4994 mL	22.4972 mL	44.9944 mL	112.4859 mL
	5 mM	0.8999 mL	4.4994 mL	8.9989 mL	22.4972 mL
	10 mM	0.4499 mL	2.2497 mL	4.4994 mL	11.2486 mL
	15 mM	0.3000 mL	1.4998 mL	2.9996 mL	7.4991 mL
	20 mM	0.2250 mL	1.1249 mL	2.2497 mL	5.6243 mL
	25 mM	0.1800 mL	0.8999 mL	1.7998 mL	4.4994 mL
	30 mM	0.1500 mL	0.7499 mL	1.4998 mL	3.7495 mL
	40 mM	0.1125 mL	0.5624 mL	1.1249 mL	2.8121 mL
	50 mM	0.0900 mL	0.4499 mL	0.8999 mL	2.2497 mL
	60 mM	0.0750 mL	0.3750 mL	0.7499 mL	1.8748 mL
	80 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4061 mL
	100 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1249 mL