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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.
分子量 | 182.22 |
公式 | C13H10O |
储存 | Desiccate at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: ZM 449829, ZM 449829 supplier, Potent, selective, JAK3, inhibitors, inhibits, JAK, Kinase, Janus, Activated, Kinases, ZM449829, AstraZeneca, 1366, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ZM 449829 的部分引用包括:
Schaertl et al (2010) A profiling platform for the characterization of transglutaminase 2 (TG2) inhibitors. J Biomol Screen 15 478 PMID: 20395409
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
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
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