420099
JAK Inhibitor I
2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI
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24 May 2012
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A potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420097) in DMSO is also available.
| Product information | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Primary Target | murine JAK1 | ||
| Primary Target IC50 | 15 nM | ||
| Secondary target | JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), Tyk2 (IC50 = 1 nM) | ||
| Molar mass | 309.3 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C18H16FN3O | ||
| CAS number | 457081-03-7 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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