BMS 509744

Biological Activity

BMS 509744 is a 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.
   Das et al.
   Bioorg.Med.Chem.Lett., 2006;16:3706
2. Selective targeting of ITK blocks multiple steps of HIV replication.
   Readinger et al.
   Proc.Natl.Acad.Sci.U.S.A., 2008;105:6684
3. 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

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