420099 Sigma-AldrichJAK Inhibitor I - CAS 457081-03-7 - Calbiochem
JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC₅₀ = 15 nM), JAK2 (IC₅₀ = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC₅₀ = 1 nM).
More>> JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC₅₀ = 15 nM), JAK2 (IC₅₀ = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC₅₀ = 1 nM). Less<<JAK Inhibitor I - CAS 457081-03-7 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
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Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 457081-03-7 | C₁₈H₁₆FN₃O |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 420099-1MG | Plastová ampulka | 1 mg | |
| 420099-500UG | Plastová ampulka | 500 μg |
| Description | |
|---|---|
| Overview | 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. |
| Catalogue Number | 420099 |
| Brand Family | Calbiochem® |
| Synonyms | 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X |
| References | |
|---|---|
| References | Pedranzini, L., et al. 2006. Cancer Res. 66, 9714. Lucet, I.S., et al. 2005. Blood 107, 176. Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 1219. |
| Product Information | |
|---|---|
| CAS number | 457081-03-7 |
| ATP Competitive | Y |
| Form | Off-white solid |
| Hill Formula | C₁₈H₁₆FN₃O |
| Chemical formula | C₁₈H₁₆FN₃O |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 420099-1MG | 04055977187878 |
| 420099-500UG | 04055977187885 |