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.
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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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