[CAS NO. 1373423-53-0] GSK-J4

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PRODUCTS SPECIFICATIONS [1373423-53-0]

Catalog

HY-15648B

Brand

MCE

CAS

1373423-53-0

DESCRIPTION [1373423-53-0]

Overview

MDL	-
Molecular Weight	417.50
Molecular Formula	C24H27N5O2
SMILES	O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1

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

24 Publications Citing Use of MCE

Summary

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC ₅₀ s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC ₅₀ of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1 ^[1] ^[2] ^[3] . GSK-J4 induces endoplasmic reticulum stress-related apoptosis ^[4] .

IC50 & Target

IC50: 8.6 µM (JMJD3/KDM6B), 6.6 µM (UTX/KDM6A) ^[6]

In Vitro

GSK-J4 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 (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 (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 inhibits JMJD3 expression that is induced by TGF-β1 ^[4] .
GSK-J4 inhibits H3K4 demethylation at Xist , Nodal , and HoxC13 in female embryonic stem cells ^[5] .

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 (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] .

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 ^[2]
Dosage:	10 mg/kg
Administration:	i.p.; thrice-weekly for 10 weeks
Result:	Attenuated the development of kidney disease in diabetic mice.

Appearance

Solid

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 : ≥ 36 mg/mL ( 86.23 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3952 mL	11.9760 mL	23.9521 mL
5 mM	0.4790 mL	2.3952 mL	4.7904 mL
10 mM	0.2395 mL	1.1976 mL	2.3952 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

* All of the co-solvents are available by MCE.