ChemicalBook Product Catalog Organic Chemistry Organic fluorine compound GSK-J4 Hydrochloride

GSK-J4 Hydrochloride

Product NameGSK-J4 Hydrochloride
CAS1797983-09-5
CBNumberCB12700565
MFC24H28ClN5O2
MW453.96442
MDL NumberMFCD26142638
MOL File1797983-09-5.mol

Chemical Properties

storage temp.	under inert gas (nitrogen or Argon) at 2-8°C
solubility	DMSO:60.83(Max Conc. mg/mL);134.0(Max Conc. mM) DMSO:PBS (pH 7.2) (1:7):0.1(Max Conc. mg/mL);0.22(Max Conc. mM) DMF:30.0(Max Conc. mg/mL);66.08(Max Conc. mM) Ethanol:55.0(Max Conc. mg/mL);121.15(Max Conc. mM) Water:10.0(Max Conc. mg/mL);22.03(Max Conc. mM)
form	A crystalline solid
color	Light yellow to yellow
InChIKey	TYXWLTBYINKVNT-UHFFFAOYSA-N
SMILES	c1(N2CCc3ccccc3CC2)cc(NCCC(=O)OCC)nc(-c2ncccc2)n1.Cl

GSK-J4 Hydrochloride Chemical Properties,Usage,Production

Description

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer. GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC₅₀ value greater than 50 μM in vitro. Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC₅₀ value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC₅₀ = 9 μM).

Uses

GSK-J4 Hydrochloride is a histone demethylase JMJD3/UTX inhibitors which blocks demethylation of histone H3K27.

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].

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.

IC 50

KDM6

References

[1] KARL AGGER. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development[J]. Nature, 2007, 449 7163: 731-734. DOI: 10.1038/nature06145
[2] M R HüBNER D L S. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation.[J]. Cold Spring Harbor symposia on quantitative biology, 2010: 43-49. DOI: 10.1101/sqb.2010.75.020
[3] LAURENS KRUIDENIER. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response[J]. Nature, 2012, 488 7411: 404-408. DOI: 10.1038/nature11262
[4] BO YANG. Reepithelialization of Diabetic Skin and Mucosal Wounds Is Rescued by Treatment With Epigenetic Inhibitors.[J]. Diabetes, 2024: 120-134. DOI: 10.2337/db23-0258

GSK-J4 Hydrochloride Supplier

Supplier	Tel	Email	Country	ProdList	Advantage
A.J Chemicals	91-9810153283	sales@ajchem.in	New Delhi，India	6052	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com		32996	60
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn		6377	58
TargetMol Chemicals Inc.	+1-781-999-5354;	support@targetmol.com		38999	58
Wuhan Topule Biopharmaceutical Co., Ltd	+86-18327326525	masar@topule.com		8432	58
HANGZHOU LEAP CHEM CO., LTD.	+86-571-87711850 +86-15355479329	market18@leapchem.com		43302	58
Aladdin Scientific		tp@aladdinsci.com		54731	58
Jiangsu Congsheng Chemical Co., Ltd.	+86-15251950002 +86-15251950002	sales4@senfeida.com		19950	58
Amadis Chemical Company Limited	571-89925085	sales@amadischem.com		131884	58
Shanghai Jijin Chemical Technology Co., Ltd.	400-002-6926 15900443528	jijinhuaxue@sina.com		6589	58

GSK-J4 Hydrochloride Spectrum

1797983-09-5(GSK-J4 Hydrochloride ) Related Search

Send Inquriy