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| Product Name: | GSK J1 | | Synonyms: | GSK J1;GSK-J1;N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine;GCK J1;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]-|-alanine;Histone Lysine Demethylase Inhibitor VII, GSK-J1;Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem | | CAS: | 1373422-53-7 | | MF: | C22H23N5O2 | | MW: | 389.45 | | EINECS: | 200-258-5 | | Product Categories: | API | | Mol File: | 1373422-53-7.mol |
| 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 |
| 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. | | 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. | | References | 1) Kruidenier et al. (2012), A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404 |
| GSK J1 Preparation Products And Raw materials |
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