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.
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All Tocris products are intended for laboratory research use only.
Crystal structures of IL-2-inducible T cell kinase complexed with inhibitors: insights into rational drug design and activity regulation.
Kutach et al.
Chem Biol Drug Des., 2010;76:154
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
Das et al.
Selective targeting of ITK blocks multiple steps of HIV replication.
Readinger et al.