GSK-J4 hydrochloride

Name: GSK-J4 hydrochloride
Brand: MedChemExpress
SKU: HY-15648F
Rating: 5.0 (37 reviews)

Cat. No.: HY-15648F Purity: 98.83%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC₅₀s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC₅₀ of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1.

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

GSK-J4 hydrochloride Chemical Structure

CAS No. : 1797983-09-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 174	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 174	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 462	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of GSK-J4 hydrochloride:

GSK-J4 In-stock

34 Publications Citing Use of MCE GSK-J4 hydrochloride

RT-PCR

: GSK-J4 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209. [Abstract]; The mRNA expression level of PKC-α is detected using qRT-PCR. GAPDH is used as an internal control.

: GSK-J4 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209. [Abstract]; After treatment with GSK-J4, the expression levels of PKC-α and p-Bcl2 in KG-1a cells are detected by Western blotting.

: GSK-J4 hydrochloride purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499. [Abstract]; Immunoblotting for H3K27me3 in cultured mouse podocytes treated with the Jmjd3 and UTX inhibitor GSK-J4 (5 μM for 48 hours) (n=3).

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•Related Screening Libraries:

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View All Histone Demethylase Isoform Specific Products:

View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

KDM6

In Vitro

GSK-J4 Hydrochloride has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α)^[1].
GSK-J4 Hydrochloride (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels^[2].
GSK-J4 Hydrochloride (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells^[3].
GSK-J4 Hydrochloride inhibits JMJD3 expression that is induced by TGF-β1^[4].
GSK-J4 Hydrochloride inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells^[5].

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

In Vivo

GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice^[2].
GSK-J4 Hydrochloride (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis^[3].

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

Animal Model:	Eight-week-old male db/m and db/db mice on a BKS background^[2]
Dosage:	10 mg/kg
Administration:	i.p.; thrice-weekly for 10 weeks
Result:	Attenuated the development of kidney disease in diabetic mice.

Molecular Weight

453.96

Formula

C₂₄H₂₈ClN₅O₂

CAS No.

1797983-09-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (137.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 3.33 mg/mL (7.34 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2028 mL	11.0142 mL	22.0284 mL
5 mM	0.4406 mL	2.2028 mL	4.4057 mL
10 mM	0.2203 mL	1.1014 mL	2.2028 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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: ≥ 2.08 mg/mL (4.58 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 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.58 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.83%

Select Batch:

Data Sheet (284 KB) SDS (251 KB)

COA (256 KB) HNMR (218 KB) LCMS (119 KB)

Handling Instructions (2659 KB)

References

[1]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. [Content Brief]

[2]. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499. [Content Brief]

[3]. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117. [Content Brief]

[4]. Yapp C, et al. H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis. Arthritis Res Ther. 2016 Jul 7;18(1):158 [Content Brief]

[5]. Kamikawa YF, et al. Histone demethylation maintains Prdm14 and Tsix expression and represses xIst in embryonic stem cells. PLoS One. 2015 May 20;10(5):e0125626 [Content Brief]

[6]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2 [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.2028 mL	11.0142 mL	22.0284 mL	55.0709 mL
H₂O / DMSO	5 mM	0.4406 mL	2.2028 mL	4.4057 mL	11.0142 mL
DMSO	10 mM	0.2203 mL	1.1014 mL	2.2028 mL	5.5071 mL
	15 mM	0.1469 mL	0.7343 mL	1.4686 mL	3.6714 mL
	20 mM	0.1101 mL	0.5507 mL	1.1014 mL	2.7535 mL
	25 mM	0.0881 mL	0.4406 mL	0.8811 mL	2.2028 mL
	30 mM	0.0734 mL	0.3671 mL	0.7343 mL	1.8357 mL
	40 mM	0.0551 mL	0.2754 mL	0.5507 mL	1.3768 mL
	50 mM	0.0441 mL	0.2203 mL	0.4406 mL	1.1014 mL
	60 mM	0.0367 mL	0.1836 mL	0.3671 mL	0.9178 mL
	80 mM	0.0275 mL	0.1377 mL	0.2754 mL	0.6884 mL
	100 mM	0.0220 mL	0.1101 mL	0.2203 mL	0.5507 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.