361559
GSK-3 Inhibitor XVI
6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile, CHIR99021
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Merck KGaA
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64293 Darmstadt
Germany
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15 Februar 2012
wird geladen
A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo.
| Produktinformationen | |||
|---|---|---|---|
| Form | Light beige solid | ||
| Protect from Light | Ja | ||
| Packaged under inert gas | Ja | ||
| Purity | ≥97% by HPLC | ||
| Chemische Formel | C22H18Cl2N8 | ||
| CAS-Nummer | 252917-06-9 | ||
| Lager- und Versandinformationen | |||
|---|---|---|---|
| Lagerkategorie | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
||
| Sicherheitshinweise | |||
|---|---|---|---|
| S-Satz |
S: 22-24/25-36-45 |
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| R-Satz |
R: 22 |
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