Potent negative allosteric modulator of LFA-1 (lymphocyte function-associated antigen-1) (Kd
= 26 nM). Binds to the I-domain of LFA-1. Reversibly inhibits LFA-1 mediated binding of SKW3 leukemia cells to ICAM-1. Inhibits superantigen (SEB)-induced IL-2 production from lymphocytes in vitro
and attenuates the SEB-induced increase in IL-2 plasma levels in a mouse model in vivo
. Orally available.
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All Tocris products are intended for laboratory research use only.
Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion.
Kelly et al.
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
Wu et al.
Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction.
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