Biological Activity
Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3) which binds competitively to the JAK3 ATP site. pIC50 values are 6.8, 5.0, 4.7, and < 5.0 for JAK3, EGFR, JAK1 and CDK4 respectively. Inhibits STAT-5 phosphorylation and T cell proliferation.
Licensing Information
Sold with the permission of AstraZeneca Ltd.
Technical Data
| M. Wt | 182.22 |
| Formula | C13H10O |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 4452-06-6 |
| PubChem ID | 3799 |
| InChI Key | FOTCGZPFSUWZBN-UHFFFAOYSA-N |
| Smiles | C=CC(C2=CC1=CC=CC=C1C=C2)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.22 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 182.22. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 5.49 mL | 27.44 mL | 54.88 mL |
| 5 mM | 1.1 mL | 5.49 mL | 10.98 mL |
| 10 mM | 0.55 mL | 2.74 mL | 5.49 mL |
| 50 mM | 0.11 mL | 0.55 mL | 1.1 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Brown et al (2000) Naphthyl ketones: a new class of janus kinase 3 inhibitors Bioorg.Med.Chem.Lett. 10 575 PMID: 10741557
Orange et al (2011) IL-2 induces a WAVE2-dependent pathway for actin reorganization that enables WASp-independent human NK cell function. J.Clin.Invest. 121 1535 PMID: 21383498
Keywords: ZM 449829, supplier, Potent, selective, JAK3, inhibitors, inhibits, JAK, Kinase, Janus, Activated, Kinases, ZM449829, AstraZeneca, JAK, Kinase, JAK, Kinase, Tocris Bioscience
