BIRT 377

Biological Activity

BIRT 377 is a potent negative allosteric modulator of LFA-1 (lymphocyte function-associated antigen-1) (K_d = 26 nM). BIRT 377 binds to the I-domain of LFA-1. BIRT 377 reversibly inhibits LFA-1 mediated binding of SKW3 leukemia cells to ICAM-1. BIRT 377 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.

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. Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
   Wu et al.
   J.Med.Chem., 2004;47:5356
2. Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion.
   Kelly et al.
   J.Immunol., 1999;163:5173
3. Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction.
   Last-Barney et al.
   J.Am.Chem.Soc., 2001;123:5643
4. Targeting the ?2-integrin LFA-1, reduces adverse neuroimmune actions in neuropathic susceptibility caused by prenatal alcohol exposure
   JJ Sanchez, JE Sanchez, S Noor, CD Ruffaner-H, S Davies, CR Wagner, LL Jantzie, N Mellios, DD Savage, ED Milligan
   Acta Neuropathol Commun, 2019;7(1):54.

Product Datasheets