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Submit ReviewZM 449829 is a 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.
Sold with the permission of AstraZeneca Ltd.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
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, ZM 449829 supplier, Potent, selective, JAK3, inhibitors, inhibits, JAK, Kinase, Janus, Activated, Kinases, ZM449829, AstraZeneca, 1366, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for ZM 449829 include:
Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478 PMID: 20395409
Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. PLoS One 10 e0143319 PMID: 26619345
Gross et al (2006) The JAK/STAT pathway is essential for opioid-induced cardioprotection: JAK2 as a mediator of STAT3, Akt, and GSK-3 beta. Am J Physiol Heart Circ Physiol 291 H827 PMID: 16517948
Lu et al (2008) JAK/STAT and PI3K/AKT pathways form a mutual transactivation loop and afford resistance to oxidative stress-induced apoptosis in cardiomyocytes. Cell Physiol Biochem 21 305 PMID: 18441519
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