Chemical Name: 4,4-Dimethyl-1-(3-nitrophenyl)-2-(1H-1,2,4-triazol-1-yl)-1-penten-3-one
Biological ActivityRab27 inhibitor (IC50 = 330 nM); inhibits Rab27a-JFC1 binding. Selectively inhibits neutrophil exocytosis, with no significant effect on other important innate immune responses including phagocytosis. Suppresses extracellular production of superoxide anion and cytochrome b plasma membrane expression. Also inhibits upregulation of adhesion molecules CD11b and CD66b. Displays in vivo anti-inflammatory activity.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of neutrophil exocytosis inhibitors (Nexinhibs), small molecule inhibitors of neutrophil exocytosis and inflammation: druggability of the small GTPase Rab27a.
Johnson et al.
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