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
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
14 February 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | Light beige solid | ||
| Molar mass | 465.3 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C22H18Cl2N8 | ||
| CAS number | 252917-06-9 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 22-24/25-36-45 Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing. In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible). |
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| R Phrase |
R: 22 Harmful if swallowed. |
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