ChemicalBook--->CAS DataBase List--->1797983-09-5

1797983-09-5

1797983-09-5 Structure

1797983-09-5 Structure
IdentificationBack Directory
[Name]

GSK-J4 Hydrochloride
[CAS]

1797983-09-5
[Synonyms]

GSK-J4 Hydrochloride
TYXWLTBYINKVNT-UHFFFAOYSA-N
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride
[Molecular Formula]

C24H28ClN5O2
[MDL Number]

MFCD26142638
[MOL File]

1797983-09-5.mol
[Molecular Weight]

453.964
Chemical PropertiesBack Directory
[storage temp. ]

Inert atmosphere,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
Safety DataBack Directory
[Symbol(GHS) ]


GHS05
[Signal word ]

Danger
[Hazard statements ]

H314-H290
[Precautionary statements ]

P501-P234-P264-P280-P390-P303+P361+P353-P301+P330+P331-P363-P304+P340+P310-P305+P351+P338+P310-P406-P405
Hazard InformationBack Directory
[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 (Item No. 12054) 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.
[storage]

Store at -20°C
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