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GSK-J1

Name: GSK-J1
Brand: TargetMol
SKU: T6847
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6847Cas No. 1373422-53-7

Alias GSK J1

GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.

GSK-J1

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Purity: 99.67%

Catalog No. T6847Alias GSK J1Cas No. 1373422-53-7

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$40	In Stock	In Stock
10 mg	$63	In Stock	In Stock
25 mg	$98	In Stock	In Stock
50 mg	$187	In Stock	In Stock
100 mg	$311	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$67	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.67%

Color:White

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Product Introduction

Bioactivity

Description	GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.
Targets&IC50	JMJD3 (KDM6B):28 nM, UTX (KDM6A):53 nM
In vitro	In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. [1] In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3. [2]
Kinase Assay	Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·Water, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.
Synonyms	GSK J1

Chemical Properties

Molecular Weight	389.45
Formula	C₂₂H₂₃N₅O₂
Cas No.	1373422-53-7
Smiles	OC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
Relative Density.	1.292 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 38.9 mg/mL (99.88 mM), Sonication is recommended.

DMSO: 250 mg/mL (641.93 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.14 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5677 mL	12.8386 mL	25.6772 mL	128.3862 mL
5 mM	0.5135 mL	2.5677 mL	5.1354 mL	25.6772 mL
10 mM	0.2568 mL	1.2839 mL	2.5677 mL	12.8386 mL
20 mM	0.1284 mL	0.6419 mL	1.2839 mL	6.4193 mL
50 mM	0.0514 mL	0.2568 mL	0.5135 mL	2.5677 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0257 mL	0.1284 mL	0.2568 mL	1.2839 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc