| 货号 | 5009/10 |
| 别名 | N-[5-[[5-[(4-Acetyl-1-piperazinyl)c |
| 供应商 | Tocris |
| 生物活性 | Potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitor (IC50 = 19 nM). Displays 200-fold selectivity over Tec family kinases and 55-fold selectivity over other kinases tested. Reduces HIV infection of primary CD4+ T cells and attenuates the establishment of HIV infection in vitro. Reduces T cell proliferation and IL-2 production in vitro. Reduces lung inflammation in a mouse model of ovalbumin-induced allergy/asthma. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >97 % |
| 计算分子量 | 623.83 |
| 分子式 | C32H41N5O4 |
| 可溶性/溶解性 | Soluble to 100 mM in 1eq. HCl and to 50 mM in DMSO |
| 参考文献 | Kutachet al (2010) Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation. Chem Biol Drug Des. 76 154. PMID: 20545945. Readingeret al (2008) Selective targeting of ITK blocks multiple steps of HIV replication. Proc.Natl.Acad.Sci.U.S.A. 105 6684. PMID: 18443296. Daset al (2006) Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. Bioorg.Med.Chem.Lett. 16 3706. PMID: 16682193. |