GSK J1 Chemical Properties

Boiling point:

608.9±55.0 °C(Predicted)

Density 

1.292±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble15mg/mL, clear

form 

powder

pka

4.20±0.10(Predicted)

color 

white to beige

Stability:

Stable for 2 years from date of purchase? as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

InChIKey

AVZCPICCWKMZDT-UHFFFAOYSA-N

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26

WGK Germany 

3

GSK J1 Usage And Synthesis

Description

GSK-J1 (1373422-53-7) is a potent and selective inhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM, human JMJD3). This is the first known inhibitor selective for the H3K27me3-specific JMJ subfamily which binds to the active catalytic site of the enzyme. The COOH group confers cell impermeability and as such GSK-J1 is useful as a standard in in vitro assays. A cell permeable ethyl ester analog is also available, see GSK-J4 (cat.# 10-1394).

Uses

GSK J1 is a selective and potent inhibitor of JMJDE and UTX demethylases.

Definition

ChEBI: 3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid is an organonitrogen heterocyclic compound.

Biochem/physiol Actions

GSK-J1 is also termed as 3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate. It may disturb the differentiation of specific neuronal subtypes in growing rat retina.

storage

room temperature (desiccate)

References

1) Kruidenier et al. (2012), A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404

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