Cat. No. 5009
Chemical Name: N-[5-[[5-[(4-Acetyl-1-piperazinyl)c
Biological ActivityPotent 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Kutach et 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.
Readinger et al (2008) Selective targeting of ITK blocks multiple steps of HIV replication. Proc.Natl.Acad.Sci.U.S.A. 105 6684. PMID: 18443296.
Das et 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.
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