| Identification | Back Directory | [Name]
GSK J1 | [CAS]
1373422-53-7 | [Synonyms]
GSK J1
GSK-J1
GCK J1
CS-2305
Histone demethylase inhibitor J1
Histone Lysine Demethylase Inhibitor VII, GSK-J1
Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyriMidinyl]-|-alanine
β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine
3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C22H23N5O2 | [MDL Number]
MFCD22683851 | [MOL File]
1373422-53-7.mol | [Molecular Weight]
389.45 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
|
|