BIRT 377 |
| رقم الكتالوجGC50078 |
BIRT 377 هو مثبط قوي متاح بيولوجيًا AMD للتفاعل بين جزيء الالتصاق بين الخلايا -1 (ICAM-1) والمستضد 1 المرتبط بوظيفة الخلايا الليمفاوية (LFA-1) ، مع Ki من 25.8 نانومتر
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Cas No.: 213211-10-0
Sample solution is provided at 25 µL, 10mM.
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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.
Kelly et al (1999) Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion. J.Immunol. 163 5173 PMID:10553036 |Wu et al (2004) Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives. J.Med.Chem. 47 5356 PMID:15481974 |Last-Barney et al (2001) Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction. J.Am.Chem.Soc. 123 5643 PMID:11403595
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