GSK-3β inhibitor 3

Name: GSK-3β inhibitor 3
Brand: MedChemExpress
SKU: HY-141480
Rating: 4.5 (1 reviews)

Cat. No.: HY-141480 Purity: 99.22%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC₅₀ of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia.

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

GSK-3β inhibitor 3 Chemical Structure

CAS No. : 1448990-73-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 275	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 275	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 375	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 675	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1010	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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GSK-3 GSK-3α GSK-3β

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

GSK-3β

6.6 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	86.3 μM Compound: 45385	Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay	[PMID: 34027661]
MOLT-4	IC₅₀	75.58 μM Compound: 45385	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay	[PMID: 34027661]
NB-4	IC₅₀	19.56 μM Compound: 45385	Cytotoxicity against human NB-4 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human NB-4 cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay	[PMID: 34027661]
NB4-DR1	IC₅₀	26.42 μM Compound: 45385	Antiproliferative activity against human NB4-DR1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human NB4-DR1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34027661]
Raji	IC₅₀	28.45 μM Compound: 45385	Cytotoxicity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by CCK-8 assay	[PMID: 34027661]

In Vitro

GSK-3β inhibitor 3 (compound 4-3) (100 μM) inhibits GSK-3α activity by 87.3%^[1].
GSK-3β inhibitor 3 (6.25-100 μM; 24-48 h) dose-dependently inhibits the growth of NB4 and NB4-R1 cells^[1].
GSK-3β inhibitor 3 (12.5-100 μM; 24 h) significantly increases the percentage of apoptosis in a dose-dependent pattern in NB4 and NB4-R1 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	NB4 and NB4-R1 cells
Concentration:	6.25, 12.5, 25, 50, 100 μM
Incubation Time:	24, 48 hours
Result:	Inhibited the cell viability, with IC₅₀s of 19.56 μM and 26.42 μM in NB4 and NB4-R1 cells at 24 h, respectively. Had little cytotoxicity on human normal liver cells (LO₂) and human umbilical vein endothelial cells (HUVECs).

Apoptosis Analysis^[1]

Cell Line:	NB4 and NB4-R1 cells
Concentration:	12.5, 25, 50, 100 μM
Incubation Time:	24 hours
Result:	Induced cell apoptosis.

In Vivo

GSK-3β inhibitor 3 (compound 4-3) (15 mg/kg/d; i.p. for 2 weeks) inhibits tumor growth of mice by 75.97% relative to vehicle control^[1].
GSK-3β inhibitor 3 (15 mg/kg; a single i.p.) shows long T_1/2 of 14.2 h, high AUC values (AUC_last=3503.42 ng/mL?h), and maximum concentration (C_max=515 ng/mL) in mice^[1].

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

Animal Model:	Balb/c female nude mice were injected leukemia cells^[1]
Dosage:	15 mg/kg/d
Administration:	I.p. for 2 weeks
Result:	Inhibited localized growth in NB4 cells. Had mild weight loss compared with control.

Animal Model:	Male ICR mice (30 g)^[1]
Dosage:	15 mg/kg (Pharmacokinetic Analysis)
Administration:	A single i.p.
Result:	T_1/2=14.2 h; AUC_last=3503.42 ng/mL•h; C_max=515 ng/mL.

Molecular Weight

327.37

Formula

C₁₈H₁₄FNO₂S

CAS No.

1448990-73-5

Appearance

Solid

Color

White to off-white

SMILES

FC(C=C1)=CC=C1C2CC(N(C(C=C)=O)C3=CC=CC=C3S2)=O

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 : 100 mg/mL (305.46 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	3.0546 mL	15.2732 mL	30.5465 mL
5 mM	0.6109 mL	3.0546 mL	6.1093 mL
10 mM	0.3055 mL	1.5273 mL	3.0546 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.

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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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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: 99.22%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (256 KB) HNMR (312 KB) RP-HPLC (269 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang P, et, al. Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. J Med Chem. 2021 May 24. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.0546 mL	15.2732 mL	30.5465 mL	76.3662 mL
	5 mM	0.6109 mL	3.0546 mL	6.1093 mL	15.2732 mL
	10 mM	0.3055 mL	1.5273 mL	3.0546 mL	7.6366 mL
	15 mM	0.2036 mL	1.0182 mL	2.0364 mL	5.0911 mL
	20 mM	0.1527 mL	0.7637 mL	1.5273 mL	3.8183 mL
	25 mM	0.1222 mL	0.6109 mL	1.2219 mL	3.0546 mL
	30 mM	0.1018 mL	0.5091 mL	1.0182 mL	2.5455 mL
	40 mM	0.0764 mL	0.3818 mL	0.7637 mL	1.9092 mL
	50 mM	0.0611 mL	0.3055 mL	0.6109 mL	1.5273 mL
	60 mM	0.0509 mL	0.2546 mL	0.5091 mL	1.2728 mL
	80 mM	0.0382 mL	0.1909 mL	0.3818 mL	0.9546 mL
	100 mM	0.0305 mL	0.1527 mL	0.3055 mL	0.7637 mL