GSK J1

Synonym(s):3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid; N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-Alanine;Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem;JHDM Inhibitor II, 3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid

CAS NO.：1373422-53-7
Empirical Formula: C22H23N5O2
Molecular Weight: 389.45
MDL number: MFCD22683851
EINECS: 200-258-5
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-07 21:39:59

What is GSK J1?

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).

The Uses of GSK J1

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

What are the applications of Application

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

Properties of GSK J1

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.

Safety information for GSK J1

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.